Dequalinium
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Identification
- Summary
Dequalinium is a quaternary ammonium cation antimicrobial agent used to treat common infections of the mouth and throat, as well as vaginal candidiasis.
- Generic Name
- Dequalinium
- DrugBank Accession Number
- DB04209
- Background
Dequalinium is an antibacterial agent with multi-targeted actions. It also possesses antifungal, antiparasitic, antiviral, anticancer, and neuroprotective properties.9 It is a quaternary ammonium compound,10 as it consists of an amphipathic cation with two aminoquinaldinium rings at both ends of a long hydrophobic hydrocarbon chain. Due to its flexible structure, dequalinium was investigated to build drug and gene delivery systems.9
First used as an antiseptic and disinfectant in the 1950s, dequalinium is still found in various OTC products to treat conditions of oral infections and inflammation.9 It is also used in vaginal tablets to treat bacterial vaginosis.10
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 456.6654
Monoisotopic: 456.3252973 - Chemical Formula
- C30H40N4
- Synonyms
- 1,1'-(1,10-Decanediyl)bis(4-amino-2-methylquinolinium) dichloride
- 1,1'-Decamethylenebis(4-aminoquinaldinium chloride)
- Decamethylenebis(4-aminoquinaldinium chloride)
- External IDs
- LSM-5846
Pharmacology
- Indication
Dequalinium is used in several OTC products to treat mouth infections and inflammation, such as tonsillitis, pharyngitis, and gingivitis.9 As vaginal tablets, dequalinium is indicated for the treatment of bacterial vaginosis in adult women under 55 years of age.10
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Bacterial vaginosis (bv) •••••••••••• ••••• •••••• Used in combination for symptomatic treatment of Breath odour Combination Product in combination with: Benzalkonium (DB11105) ••• ••• •••••••• Used in combination to treat Gingivitis Combination Product in combination with: Benzalkonium (DB11105) ••• ••• •••••••• Treatment of Inflammation of mouth ••• ••• Used in combination to treat Inflammation of mouth Combination Product in combination with: Benzalkonium (DB11105) ••• ••• •••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
In vitro, dequalinium possesses antimicrobial activity against gram-positive and gram-negative bacteria, yeasts, and protozoa.6 Dequalinium has a rapid bactericidal and fungicidal action.1 The antiparasitic and antiviral properties of dequalinium have also been noted. For example, dequalinium can bind to the membrane-proximal external region (MPER) of the spike envelope of the human immunodeficiency virus HIV-1.9
As with other quaternary ammonium compounds similar to dequalinium, gram-positive bacteria are more sensitive to dequalinium than gram-negative bacteria.6,10 The bactericidal and fungicidal effects of dequalinium can occur within 30 to 60 minutes.7 According to in vitro studies, the minimal inhibitory concentration (MIC) for dequalinium against relevant vaginal pathogens ranges from 0.2 to ≥ 1024 µg/mL.10
There is evidence that dequalinium exhibits anticancer activity in human leukemia cells: dequalinium induces a cytotoxic effect by altering redox balance, downregulating Raf/MEK/ERK1/2 and PI3K/Akt signalling pathways, and promoting apoptosis of leukemic cells.3,4,5 Dequalinium was also shown to block small conductance Ca2+-activated K+ channels, called SK channels, which are often expressed in some cancer cells to play a role in cell proliferation and migration.9 One study showed that dequalinium reduced macrophage motility in mice, inhibiting macrophage infiltration of irradiated tumours and attenuating local metastasis.2
Interestingly, dequalinium was shown to modulate and induce self-oligomerization of alpha-synuclein, a synaptic protein known to cause aggregates in several neurodegenerative disorders. This finding highlights the neuroprotective actions of dequalinium; however, further investigations are warranted as dequalinium is a neurotoxic agent.9
- Mechanism of action
Dequalinium has multiple modes of action. Dequalinium absorbs into the bacterial cell surface and diffuses through the cell wall, disrupting bacterial cell permeability.6,9 It is taken up by the bacteria rapidly.9 Once in the bacteria, dequalinium denatures proteins involved in the respiratory chain and glycolysis of bacteria, interfering with bacterial cell metabolism and ribosomal protein synthesis.1,6,9 By inhibiting bacterial F1-ATPase, dequalinium inhibits mitochondrial ATP synthesis and blocks glucose metabolism. These molecular actions ultimately deplete bacterial energy sources.1 As dequalinium accumulates in the mitochondria, it is considered a mitochondrial poison.8,9
Dequalinium can also precipitate nucleic acids, as it can intercalate one of its quinoline chromophores between DNA base pairs.1,9 Depending on the drug concentration, dequalinium can lyse the bacterial cell by promoting osmotic imbalance.1,6
Target Actions Organism ASmall conductance calcium-activated potassium channel protein 1 blockerHumans ACyclic nucleotide-gated channel alpha-2 blockerHumans ASmall conductance calcium-activated potassium channel protein 2 blockerHumans AE3 ubiquitin-protein ligase XIAP antagonistinhibitorHumans ACyclic nucleotide-gated channel alpha-1 blockerHumans ASmall conductance calcium-activated potassium channel protein 3 blockerHumans UCalcium-activated potassium channel subunit alpha-1 inhibitorHumans UHTH-type transcriptional regulator QacR regulatorStaphylococcus aureus UResponse regulator RamR regulatorStreptomyces coelicolor (strain ATCC BAA-471 / A3(2) / M145) UProtein kinase C inhibitorHumans UAlpha-synuclein modulatorHumans UL-cysteine:1D-myo-inositol 2-amino-2-deoxy-alpha-D-glucopyranoside ligase inhibitorMycobacterium tuberculosis (strain ATCC 25177 / H37Ra) UCalmodulin antagonistHumans - Absorption
Following vaginal administration, dequalinium is not readily absorbed into the systemic circulation. The concentration of dequalinium chloride in vaginal fluid was 2000 to 4000 mg/L in vitro after dissolution of one vaginal tablet (equivalent of 10 mg dequalinium chloride) in an estimated 2.5 to 5 mg/L of vaginal fluid.10
- Volume of distribution
There is no information available.
- Protein binding
There is no information available.
- Metabolism
There is no information available.
- Route of elimination
There is no information available.
- Half-life
There is no information available.
- Clearance
There is no information available.
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
The LD50 was 18300 ug/kg following intraperitoneal administration and 70 mg/kg following subcutaneous administration in mice.11 There is limited clinical experience of drug overdose with dequalinium. While dequalinium is generally well tolerated and considered as safe at recommended therapeutic doses, dequalinium is a neurotoxic agent and mitochondrial poison. At a high dose in mice, the drug caused damages to the liver and kidneys, and caused renal and hepatic failure.9
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcenocoumarol The risk or severity of bleeding can be increased when Dequalinium is combined with Acenocoumarol. Ambroxol The risk or severity of methemoglobinemia can be increased when Dequalinium is combined with Ambroxol. Articaine The risk or severity of methemoglobinemia can be increased when Dequalinium is combined with Articaine. BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Dequalinium. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Dequalinium is combined with Benzyl alcohol. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Dequalinium acetate P8W4UX112S 4028-98-2 IWYNVAJACBPVLT-UHFFFAOYSA-N Dequalinium bromide Not Available Not Available Not applicable Dequalinium chloride XYS8INN1I6 522-51-0 LTNZEXKYNRNOGT-UHFFFAOYSA-N Dequalinium iodide Not Available Not Available Not applicable Dequalinium undecenoate Not Available Not Available Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Vablys Tablet 10 mg Vaginal Duchesnay Inc. 2022-05-17 Not applicable Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image AXCEL DEXXON LOZENGES Lozenge Oral KOTRA PHARMA (M) SDN. BHD. 2020-09-08 Not applicable Malaysia Citrex DQM Lozenges Lemon Ginger 0.25mg Lozenge 0.25 mg Oral IDAMAN PHARMA MANUFACTURING SDN BHD 2020-09-08 2021-12-12 Malaysia Citrex DQM Lozenges Lemon Honey 0.25mg Lozenge 0.25 mg Oral IDAMAN PHARMA MANUFACTURING SDN BHD 2020-09-08 2024-02-24 Malaysia Citrex DQM Lozenges Orange 0.25mg Lozenge 0.25 mg Oral IDAMAN PHARMA MANUFACTURING SDN BHD 2020-09-08 2024-02-24 Malaysia DELIN Lozenge 0.25 mg Oral บริษัท โรงงานเภสัชกรรมแอตแลนติค จำกัด 2020-06-22 Not applicable Thailand - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BUCOSEPTOL® TABLETAS Dequalinium chloride (0.25 mg) + Benzocaine (15 mg) Tablet Oral LABORATORIOS NEOLTDA. 2013-03-05 2013-05-23 Colombia CEQUALIN Dequalinium chloride (250 mcg) + Ascorbic acid (51.55 mg) Lozenge Oral Erlangga Edi Laboratories (Erela) 2018-03-29 2025-02-01 Indonesia DECATYLEN LOZENGE Dequalinium chloride (0.25 mg) + Cinchocaine hydrochloride (0.03 mg) Lozenge Oral APEX PHARMA MARKETING PTE. LTD. 1990-06-25 Not applicable Singapore DECATYLEN LOZENGES Dequalinium chloride (0.25 mg) + Cinchocaine hydrochloride (0.03 mg) Lozenge Oral MEPHARM (MALAYSIA) SDN. BHD. 2020-09-08 2024-06-28 Malaysia DEQ LOZENGE Dequalinium chloride (0.25 mg) + Tyrothricin (1 mg) Tablet Oral ATLANTIC PHARMACEUTICAL (S) PTE LTD 1990-01-13 Not applicable Singapore
Categories
- ATC Codes
- D08AH01 — Dequalinium
- D08AH — Quinoline derivatives
- D08A — ANTISEPTICS AND DISINFECTANTS
- D08 — ANTISEPTICS AND DISINFECTANTS
- D — DERMATOLOGICALS
- Drug Categories
- Anti-Bacterial Agents
- Anti-Infective Agents
- Anti-Infective Agents, Local
- Antiseptics and Disinfectants
- Dermatologicals
- Genito Urinary System and Sex Hormones
- Gynecological Antiinfectives and Antiseptics
- Heterocyclic Compounds, Fused-Ring
- Miscellaneous Anti-infectives
- Quinoline Derivatives
- Quinolines
- Quinolinium Compounds
- Throat Preparations
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 4-aminoquinolines. These are organic compounds containing an amino group attached to the 4-position of a quinoline ring system.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Quinolines and derivatives
- Sub Class
- Aminoquinolines and derivatives
- Direct Parent
- 4-aminoquinolines
- Alternative Parents
- Methylpyridines / Aminopyridines and derivatives / Pyridinium derivatives / Benzenoids / Heteroaromatic compounds / Azacyclic compounds / Primary amines / Organopnictogen compounds / Hydrocarbon derivatives / Organic cations
- Substituents
- 4-aminoquinoline / Amine / Aminopyridine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Heteroaromatic compound / Hydrocarbon derivative / Methylpyridine / Organic cation
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- quinolinium ion (CHEBI:41872)
- Affected organisms
- Candida albicans and other yeasts
- Trichomonas vaginalis, Giardia duodenalis, and Entamoeba histolytica
- Bacteria and protozoa
- Bacteroides
- Peptostreptococcus
Chemical Identifiers
- UNII
- E7QC7V26B8
- CAS number
- 6707-58-0
- InChI Key
- PCSWXVJAIHCTMO-UHFFFAOYSA-P
- InChI
- InChI=1S/C30H38N4/c1-23-21-27(31)25-15-9-11-17-29(25)33(23)19-13-7-5-3-4-6-8-14-20-34-24(2)22-28(32)26-16-10-12-18-30(26)34/h9-12,15-18,21-22,31-32H,3-8,13-14,19-20H2,1-2H3/p+2
- IUPAC Name
- 4-amino-1-[10-(4-amino-2-methylquinolin-1-ium-1-yl)decyl]-2-methylquinolin-1-ium
- SMILES
- CC1=CC(N)=C2C=CC=CC2=[N+]1CCCCCCCCCC[N+]1=C(C)C=C(N)C2=C1C=CC=C2
References
- General References
- Mendling W, Weissenbacher ER, Gerber S, Prasauskas V, Grob P: Use of locally delivered dequalinium chloride in the treatment of vaginal infections: a review. Arch Gynecol Obstet. 2016 Mar;293(3):469-84. doi: 10.1007/s00404-015-3914-8. Epub 2015 Oct 27. [Article]
- Timaner M, Bril R, Kaidar-Person O, Rachman-Tzemah C, Alishekevitz D, Kotsofruk R, Miller V, Nevelsky A, Daniel S, Raviv Z, Rotenberg SA, Shaked Y: Dequalinium blocks macrophage-induced metastasis following local radiation. Oncotarget. 2015 Sep 29;6(29):27537-54. doi: 10.18632/oncotarget.4826. [Article]
- Sancho P, Galeano E, Estan MC, Ganan-Gomez I, Boyano-Adanez Mdel C, Garcia-Perez AI: Raf/MEK/ERK signaling inhibition enhances the ability of dequalinium to induce apoptosis in the human leukemic cell line K562. Exp Biol Med (Maywood). 2012 Aug;237(8):933-42. doi: 10.1258/ebm.2012.011423. Epub 2012 Aug 8. [Article]
- Garcia-Perez AI, Galeano E, Nieto E, Sancho P: Dequalinium induces human leukemia cell death by affecting the redox balance. Leuk Res. 2011 Oct;35(10):1395-401. doi: 10.1016/j.leukres.2011.03.012. Epub 2011 Apr 8. [Article]
- Garcia-Perez AI, Galeano E, Nieto E, Estan MC, Sancho P: Dequalinium induces cytotoxicity in human leukemia NB4 cells by downregulation of Raf/MEK/ERK and PI3K/Akt signaling pathways and potentiation of specific inhibitors of these pathways. Leuk Res. 2014 Jul;38(7):795-803. doi: 10.1016/j.leukres.2014.01.009. Epub 2014 Jan 28. [Article]
- Della Casa V, Noll H, Gonser S, Grob P, Graf F, Pohlig G: Antimicrobial activity of dequalinium chloride against leading germs of vaginal infections. Arzneimittelforschung. 2002;52(9):699-705. [Article]
- D'Auria FD, Simonetti G, Strippoli V: [Antimicrobial characteristics of a tincture of dequalinium chloride]. Ann Ig. 1989 Sep-Oct;1(5):1227-41. [Article]
- Weiss MJ, Wong JR, Ha CS, Bleday R, Salem RR, Steele GD Jr, Chen LB: Dequalinium, a topical antimicrobial agent, displays anticarcinoma activity based on selective mitochondrial accumulation. Proc Natl Acad Sci U S A. 1987 Aug;84(15):5444-8. [Article]
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
- Health Canada Approved Drug Products: VABLYS (Dequalinium) Vaginal Tablets [Link]
- Cayman Chemical: Dequalinium MSDS [Link]
- External Links
- PubChem Compound
- 2993
- PubChem Substance
- 46507206
- ChemSpider
- 2886
- BindingDB
- 50048403
- 3226
- ChEBI
- 41872
- ChEMBL
- CHEMBL333826
- ZINC
- ZINC000001655706
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- DEQ
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Dequalinium
- PDB Entries
- 1jt6 / 1oyd / 3arp / 3art / 3br1 / 3br2 / 3bt9 / 3btj / 3vw0
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Bacterial Vaginoses 1 somestatus stop reason just information to hide 4 Completed Treatment Vulvovaginal Candidiasis 1 somestatus stop reason just information to hide 4 Terminated Treatment Bacterial Vaginosis (BV) / Vaginal Diseases / Vaginal Infections 1 somestatus stop reason just information to hide 3 Completed Treatment Bacterial Vaginosis (BV) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral Lozenge Oral 0254 MG Lozenge Oral 0.25 mg Tablet Oral 0.25 mg Lozenge Oral Lozenge Oral 250 mcg Solution Oral Spray Oral Lozenge Oral .25 mg / loz Solution Buccal 0.5 % w/v Liquid Oral 0.5 % Tablet Oral 0.25 mg Solution Oral Insert Vaginal 10 mg Solution Topical 5 mg/mL Lozenge Oral 25 mg Ointment Topical Tablet Vaginal Tablet Vaginal 10 mg Pastille Oral Pastille Oral Tablet Vaginal 10.000 mg Lozenge Oral Solution Oral 1 mg/10ml Lozenge Oral 0.25 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US4946849 No 1990-08-07 2002-10-01 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source boiling point (°C) 300 https://datasheets.scbt.com/sds/aghs/en/sc-214869.pdf - Predicted Properties
Property Value Source Water Solubility 4.77e-07 mg/mL ALOGPS logP 0.16 ALOGPS logP -3.6 Chemaxon logS -9 ALOGPS pKa (Strongest Basic) -0.34 Chemaxon Physiological Charge 2 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 59.8 Å2 Chemaxon Rotatable Bond Count 11 Chemaxon Refractivity 147 m3·mol-1 Chemaxon Polarizability 56.76 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.5208 Blood Brain Barrier + 0.924 Caco-2 permeable + 0.5756 P-glycoprotein substrate Substrate 0.6725 P-glycoprotein inhibitor I Non-inhibitor 0.7203 P-glycoprotein inhibitor II Inhibitor 0.7281 Renal organic cation transporter Inhibitor 0.6769 CYP450 2C9 substrate Non-substrate 0.8745 CYP450 2D6 substrate Non-substrate 0.5072 CYP450 3A4 substrate Non-substrate 0.5434 CYP450 1A2 substrate Non-inhibitor 0.6703 CYP450 2C9 inhibitor Non-inhibitor 0.9119 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Inhibitor 0.6677 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5512 Ames test AMES toxic 0.5875 Carcinogenicity Non-carcinogens 0.9063 Biodegradation Not ready biodegradable 0.9969 Rat acute toxicity 2.6736 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.823 hERG inhibition (predictor II) Inhibitor 0.9123
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 247.722742 predictedDarkChem Lite v0.1.0 [M-H]- 210.51427 predictedDeepCCS 1.0 (2019) [M+H]+ 250.236742 predictedDarkChem Lite v0.1.0 [M+H]+ 212.87224 predictedDeepCCS 1.0 (2019) [M+Na]+ 247.766642 predictedDarkChem Lite v0.1.0 [M+Na]+ 218.9654 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Blocker
- General Function
- Small conductance calcium-activated potassium channel that mediates the voltage-independent transmembrane transfer of potassium across the cell membrane through a constitutive interaction with calmodulin which binds the intracellular calcium allowing its opening (PubMed:17142458, PubMed:8781233, PubMed:9287325). The current is characterized by a voltage-independent activation, an intracellular calcium concentration increase-dependent activation and a single-channel conductance of about 3 picosiemens (PubMed:8781233). Also presents an inwardly rectifying current, thus reducing its already small outward conductance of potassium ions, which is particularly the case when the membrane potential displays positive values, above + 20 mV (Probable). Activation is followed by membrane hyperpolarization (By similarity). Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization (By similarity)
- Specific Function
- calcium-activated potassium channel activity
- Gene Name
- KCNN1
- Uniprot ID
- Q92952
- Uniprot Name
- Small conductance calcium-activated potassium channel protein 1
- Molecular Weight
- 59986.87 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Blocker
- General Function
- Pore-forming subunit of the olfactory cyclic nucleotide-gated channel. Operates in the cilia of olfactory sensory neurons where chemical stimulation of the odorant is converted to an electrical signal. Mediates odorant-induced cAMP-dependent Ca(2+) influx triggering neuron depolarization. The rise of intracellular Ca(2+) levels potentiates the olfactory response by activating Ca(2+)-dependent Cl(-) channels, but it also serves as a negative feedback signal to desensitize the channel for rapid adaptation to odorants. Conducts cAMP- and cGMP-gated ion currents, with permeability for monovalent and divalent cations
- Specific Function
- calcium channel activity
- Gene Name
- CNGA2
- Uniprot ID
- Q16280
- Uniprot Name
- Cyclic nucleotide-gated channel alpha-2
- Molecular Weight
- 76047.505 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Blocker
- General Function
- Small conductance calcium-activated potassium channel that mediates the voltage-independent transmembrane transfer of potassium across the cell membrane through a constitutive interaction with calmodulin which binds the intracellular calcium allowing its opening (PubMed:10991935, PubMed:33242881, PubMed:9287325). The current is characterized by a voltage-independent activation, an intracellular calcium concentration increase-dependent activation and a single-channel conductance of about 3 picosiemens (PubMed:10991935). Also presents an inwardly rectifying current, thus reducing its already small outward conductance of potassium ions, which is particularly the case when the membrane potential displays positive values, above + 20 mV (PubMed:10991935). The inward rectification could be due to a blockade of the outward current by intracellular divalent cations such as calcium and magnesium and could also be due to an intrinsic property of the channel pore, independent of intracellular divalent ions. There are three positively charged amino acids in the S6 transmembrane domain, close to the pore, that collectively control the conductance and rectification through an electrostatic mechanism. Additionally, electrostatic contributions from these residues also play an important role in determining the intrinsic open probability of the channel in the absence of calcium, affecting the apparent calcium affinity for activation. Forms an heteromeric complex with calmodulin, which is constitutively associated in a calcium-independent manner. Channel opening is triggered when calcium binds the calmodulin resulting in a rotary movement leading to the formation of the dimeric complex to open the gate (By similarity). Plays a role in the repolarization phase of cardiac action potential (PubMed:13679367)
- Specific Function
- alpha-actinin binding
- Gene Name
- KCNN2
- Uniprot ID
- Q9H2S1
- Uniprot Name
- Small conductance calcium-activated potassium channel protein 2
- Molecular Weight
- 63759.03 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntagonistInhibitor
- General Function
- Multi-functional protein which regulates not only caspases and apoptosis, but also modulates inflammatory signaling and immunity, copper homeostasis, mitogenic kinase signaling, cell proliferation, as well as cell invasion and metastasis (PubMed:11257230, PubMed:11257231, PubMed:11447297, PubMed:12121969, PubMed:12620238, PubMed:17560374, PubMed:17967870, PubMed:19473982, PubMed:20154138, PubMed:22103349, PubMed:9230442). Acts as a direct caspase inhibitor (PubMed:11257230, PubMed:11257231, PubMed:12620238). Directly bind to the active site pocket of CASP3 and CASP7 and obstructs substrate entry (PubMed:11257230, PubMed:11257231, PubMed:16352606, PubMed:16916640). Inactivates CASP9 by keeping it in a monomeric, inactive state (PubMed:12620238). Acts as an E3 ubiquitin-protein ligase regulating NF-kappa-B signaling and the target proteins for its E3 ubiquitin-protein ligase activity include: RIPK1, RIPK2, MAP3K2/MEKK2, DIABLO/SMAC, AIFM1, CCS, PTEN and BIRC5/survivin (PubMed:17560374, PubMed:17967870, PubMed:19473982, PubMed:20154138, PubMed:22103349, PubMed:22607974, PubMed:29452636, PubMed:30026309). Acts as an important regulator of innate immunity by mediating 'Lys-63'-linked polyubiquitination of RIPK2 downstream of NOD1 and NOD2, thereby transforming RIPK2 into a scaffolding protein for downstream effectors, ultimately leading to activation of the NF-kappa-B and MAP kinases signaling (PubMed:19667203, PubMed:22607974, PubMed:29452636, PubMed:30026309). 'Lys-63'-linked polyubiquitination of RIPK2 also promotes recruitment of the LUBAC complex to RIPK2 (PubMed:22607974, PubMed:29452636). Regulates the BMP signaling pathway and the SMAD and MAP3K7/TAK1 dependent pathways leading to NF-kappa-B and JNK activation (PubMed:17560374). Ubiquitination of CCS leads to enhancement of its chaperone activity toward its physiologic target, SOD1, rather than proteasomal degradation (PubMed:20154138). Ubiquitination of MAP3K2/MEKK2 and AIFM1 does not lead to proteasomal degradation (PubMed:17967870, PubMed:22103349). Plays a role in copper homeostasis by ubiquitinating COMMD1 and promoting its proteasomal degradation (PubMed:14685266). Can also function as E3 ubiquitin-protein ligase of the NEDD8 conjugation pathway, targeting effector caspases for neddylation and inactivation (PubMed:21145488). Ubiquitinates and therefore mediates the proteasomal degradation of BCL2 in response to apoptosis (PubMed:29020630). Protects cells from spontaneous formation of the ripoptosome, a large multi-protein complex that has the capability to kill cancer cells in a caspase-dependent and caspase-independent manner (PubMed:22095281). Suppresses ripoptosome formation by ubiquitinating RIPK1 and CASP8 (PubMed:22095281). Acts as a positive regulator of Wnt signaling and ubiquitinates TLE1, TLE2, TLE3, TLE4 and AES (PubMed:22304967). Ubiquitination of TLE3 results in inhibition of its interaction with TCF7L2/TCF4 thereby allowing efficient recruitment and binding of the transcriptional coactivator beta-catenin to TCF7L2/TCF4 that is required to initiate a Wnt-specific transcriptional program (PubMed:22304967)
- Specific Function
- cysteine-type endopeptidase inhibitor activity
- Gene Name
- XIAP
- Uniprot ID
- P98170
- Uniprot Name
- E3 ubiquitin-protein ligase XIAP
- Molecular Weight
- 56684.41 Da
References
- Orzaez M, Gortat A, Sancho M, Carbajo RJ, Pineda-Lucena A, Palacios-Rodriguez Y, Perez-Paya E: Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain. Apoptosis. 2011 May;16(5):460-7. doi: 10.1007/s10495-011-0582-4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Blocker
- General Function
- Pore-forming subunit of the rod cyclic nucleotide-gated channel. Mediates rod photoresponses at dim light converting transient changes in intracellular cGMP levels into electrical signals. In the dark, cGMP levels are high and keep the channel open enabling a steady inward current carried by Na(+) and Ca(2+) ions that leads to membrane depolarization and neurotransmitter release from synaptic terminals. Upon photon absorption cGMP levels decline leading to channel closure and membrane hyperpolarization that ultimately slows neurotransmitter release and signals the presence of light, the end point of the phototransduction cascade. Conducts cGMP- and cAMP-gated ion currents, with permeability for monovalent and divalent cations. The selectivity for Ca(2+) over Na(+) increases with cGMP concentrations, whereas the selectivity among monovalent ions is independent of the cGMP levels
- Specific Function
- calcium channel activity
- Gene Name
- CNGA1
- Uniprot ID
- P29973
- Uniprot Name
- Cyclic nucleotide-gated channel alpha-1
- Molecular Weight
- 79125.225 Da
References
- Rosenbaum T, Islas LD, Carlson AE, Gordon SE: Dequalinium: a novel, high-affinity blocker of CNGA1 channels. J Gen Physiol. 2003 Jan;121(1):37-47. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Blocker
- General Function
- Small conductance calcium-activated potassium channel that mediates the voltage-independent transmembrane transfer of potassium across the cell membrane through a constitutive interaction with calmodulin which binds the intracellular calcium allowing its opening (PubMed:12808432, PubMed:20562108, PubMed:31155282, PubMed:36502918). The current is characterized by a voltage-independent activation, an intracellular calcium concentration increase-dependent activation and a single-channel conductance of 10 picosiemens (PubMed:12808432, PubMed:20562108, PubMed:31155282, PubMed:36502918). Also presents an inwardly rectifying current, thus reducing its already small outward conductance of potassium ions, which is particularly the case when the membrane potential displays positive values, above + 20 mV (PubMed:12808432). Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization (By similarity)
- Specific Function
- calmodulin binding
- Gene Name
- KCNN3
- Uniprot ID
- Q9UGI6
- Uniprot Name
- Small conductance calcium-activated potassium channel protein 3
- Molecular Weight
- 81384.63 Da
References
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+) (PubMed:14523450, PubMed:29330545, PubMed:31152168). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX)
- Specific Function
- actin binding
- Gene Name
- KCNMA1
- Uniprot ID
- Q12791
- Uniprot Name
- Calcium-activated potassium channel subunit alpha-1
- Molecular Weight
- 137558.115 Da
References
- Castle NA, Haylett DG, Morgan JM, Jenkinson DH: Dequalinium: a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle. Eur J Pharmacol. 1993 May 19;236(2):201-7. [Article]
- Kind
- Protein
- Organism
- Staphylococcus aureus
- Pharmacological action
- Unknown
- Actions
- Regulator
- General Function
- Transcriptional repressor of qacA. Binds to IR1, an unusually long 28 bp operator, which is located downstream from the qacA promoter and overlaps its transcription start site. QacR is induced from its IR1 site by binding to one of many structurally dissimilar cationic lipophilic compounds, which are also substrates of QacA.
- Specific Function
- DNA binding
- Gene Name
- qacR
- Uniprot ID
- P0A0N4
- Uniprot Name
- HTH-type transcriptional regulator QacR
- Molecular Weight
- 22174.175 Da
References
- Peters KM, Schuman JT, Skurray RA, Brown MH, Brennan RG, Schumacher MA: QacR-cation recognition is mediated by a redundancy of residues capable of charge neutralization. Biochemistry. 2008 Aug 5;47(31):8122-9. doi: 10.1021/bi8008246. Epub 2008 Jul 11. [Article]
- Murray DS, Schumacher MA, Brennan RG: Crystal structures of QacR-diamidine complexes reveal additional multidrug-binding modes and a novel mechanism of drug charge neutralization. J Biol Chem. 2004 Apr 2;279(14):14365-71. doi: 10.1074/jbc.M313870200. Epub 2004 Jan 15. [Article]
- Kind
- Protein
- Organism
- Streptomyces coelicolor (strain ATCC BAA-471 / A3(2) / M145)
- Pharmacological action
- Unknown
- Actions
- Regulator
- General Function
- A transcription factor required for aerial hyphae formation on rich medium (PubMed:12100547, PubMed:12453210). Activates transcription of ramC. Might be part of a two-component regulatory system (PubMed:12453210). Binds the promoter of ramC (PubMed:12100547, PubMed:12453210). Non-phosphorylated protein cooperatively binds multiple sites in the ramC promoter. Has not been seen to autophosphorylate using the small molecule phosphodonors phosphoramidate, acetyl phosphate or carbamoyl phosphate (PubMed:16051268). Upon low expression suppresses the bald (bld, no aerial hyphae) phenotype of citA but not bldJ mutants; higher expression also suppresses the bldJ mutant as well as several other bld mutations, inducing SapB production even on media where SapB is normally not produced (PubMed:12453210). Expression of the ram locus (ramA, ramB and ramR) induces rapid aerial mycelium formation in S.lividans (PubMed:8206859). Overexpression suppresses the no aerial hyphae phenotype of a chaplin-negative strain, probably by inducing expression of SapB (PubMed:17462011). Overexpression of RamR show there are about 280 genes having at least a threefold increase or fourfold decrease in RNA abundance versus wild-type including gene cluster SCO4072-SCO4075 (PubMed:16925552).
- Specific Function
- DNA binding
- Gene Name
- ramR
- Uniprot ID
- Q7AKE4
- Uniprot Name
- Response regulator RamR
- Molecular Weight
- 21489.545 Da
References
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in positive and negative regulation of cell proliferation, apoptosis, differentiation, migration and adhesion, tumorigenesis, cardiac hypertrophy, angiogenesis, platelet function and inflammation, by directly phosphorylating targets such as RAF1, BCL2, CSPG4, TNNT2/CTNT, or activating signaling cascade involving MAPK1/3 (ERK1/2) and RAP1GAP. Involved in cell proliferation and cell growth arrest by positive and negative regulation of the cell cycle. Can promote cell growth by phosphorylating and activating RAF1, which mediates the activation of the MAPK/ERK signaling cascade, and/or by up-regulating CDKN1A, which facilitates active cyclin-dependent kinase (CDK) complex formation in glioma cells. In intestinal cells stimulated by the phorbol ester PMA, can trigger a cell cycle arrest program which is associated with the accumulation of the hyper-phosphorylated growth-suppressive form of RB1 and induction of the CDK inhibitors CDKN1A and CDKN1B. Exhibits anti-apoptotic function in glioma cells and protects them from apoptosis by suppressing the p53/TP53-mediated activation of IGFBP3, and in leukemia cells mediates anti-apoptotic action by phosphorylating BCL2. During macrophage differentiation induced by macrophage colony-stimulating factor (CSF1), is translocated to the nucleus and is associated with macrophage development. After wounding, translocates from focal contacts to lamellipodia and participates in the modulation of desmosomal adhesion. Plays a role in cell motility by phosphorylating CSPG4, which induces association of CSPG4 with extensive lamellipodia at the cell periphery and polarization of the cell accompanied by increases in cell motility. During chemokine-induced CD4(+) T cell migration, phosphorylates CDC42-guanine exchange factor DOCK8 resulting in its dissociation from LRCH1 and the activation of GTPase CDC42 (PubMed:28028151). Is highly expressed in a number of cancer cells where it can act as a tumor promoter and is implicated in malignant phenotypes of several tumors such as gliomas and breast cancers. Negatively regulates myocardial contractility and positively regulates angiogenesis, platelet aggregation and thrombus formation in arteries. Mediates hypertrophic growth of neonatal cardiomyocytes, in part through a MAPK1/3 (ERK1/2)-dependent signaling pathway, and upon PMA treatment, is required to induce cardiomyocyte hypertrophy up to heart failure and death, by increasing protein synthesis, protein-DNA ratio and cell surface area. Regulates cardiomyocyte function by phosphorylating cardiac troponin T (TNNT2/CTNT), which induces significant reduction in actomyosin ATPase activity, myofilament calcium sensitivity and myocardial contractility. In angiogenesis, is required for full endothelial cell migration, adhesion to vitronectin (VTN), and vascular endothelial growth factor A (VEGFA)-dependent regulation of kinase activation and vascular tube formation. Involved in the stabilization of VEGFA mRNA at post-transcriptional level and mediates VEGFA-induced cell proliferation. In the regulation of calcium-induced platelet aggregation, mediates signals from the CD36/GP4 receptor for granule release, and activates the integrin heterodimer ITGA2B-ITGB3 through the RAP1GAP pathway for adhesion. During response to lipopolysaccharides (LPS), may regulate selective LPS-induced macrophage functions involved in host defense and inflammation. But in some inflammatory responses, may negatively regulate NF-kappa-B-induced genes, through IL1A-dependent induction of NF-kappa-B inhibitor alpha (NFKBIA/IKBA). Upon stimulation with 12-O-tetradecanoylphorbol-13-acetate (TPA), phosphorylates EIF4G1, which modulates EIF4G1 binding to MKNK1 and may be involved in the regulation of EIF4E phosphorylation. Phosphorylates KIT, leading to inhibition of KIT activity. Phosphorylates ATF2 which promotes cooperation between ATF2 and JUN, activating transcription. Phosphorylates SOCS2 at 'Ser-52' facilitating its ubiquitination and proteasomal degradation (By similarity). Phosphorylates KLHL3 in response to angiotensin II signaling, decreasing the interaction between KLHL3 and WNK4 (PubMed:25313067). Phosphorylates and activates LRRK1, which phosphorylates RAB proteins involved in intracellular trafficking (PubMed:36040231)
- Specific Function
- ATP binding
Components:
References
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Modulator
- General Function
- Neuronal protein that plays several roles in synaptic activity such as regulation of synaptic vesicle trafficking and subsequent neurotransmitter release (PubMed:20798282, PubMed:26442590, PubMed:28288128, PubMed:30404828). Participates as a monomer in synaptic vesicle exocytosis by enhancing vesicle priming, fusion and dilation of exocytotic fusion pores (PubMed:28288128, PubMed:30404828). Mechanistically, acts by increasing local Ca(2+) release from microdomains which is essential for the enhancement of ATP-induced exocytosis (PubMed:30404828). Acts also as a molecular chaperone in its multimeric membrane-bound state, assisting in the folding of synaptic fusion components called SNAREs (Soluble NSF Attachment Protein REceptors) at presynaptic plasma membrane in conjunction with cysteine string protein-alpha/DNAJC5 (PubMed:20798282). This chaperone activity is important to sustain normal SNARE-complex assembly during aging (PubMed:20798282). Also plays a role in the regulation of the dopamine neurotransmission by associating with the dopamine transporter (DAT1) and thereby modulating its activity (PubMed:26442590)
- Specific Function
- actin binding
- Gene Name
- SNCA
- Uniprot ID
- P37840
- Uniprot Name
- Alpha-synuclein
- Molecular Weight
- 14460.155 Da
References
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
- Kind
- Protein
- Organism
- Mycobacterium tuberculosis (strain ATCC 25177 / H37Ra)
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Dequalinium inhibits this enzyme, also known as mycothiol ligase (MshC).
- General Function
- Catalyzes the ATP-dependent condensation of GlcN-Ins and L-cysteine to form L-Cys-GlcN-Ins.
- Specific Function
- ATP binding
- Gene Name
- mshC
- Uniprot ID
- A5U4F6
- Uniprot Name
- L-cysteine:1D-myo-inositol 2-amino-2-deoxy-alpha-D-glucopyranoside ligase
- Molecular Weight
- 45594.045 Da
References
- Gutierrez-Lugo MT, Baker H, Shiloach J, Boshoff H, Bewley CA: Dequalinium, a new inhibitor of Mycobacterium tuberculosis mycothiol ligase identified by high-throughput screening. J Biomol Screen. 2009 Jul;14(6):643-52. doi: 10.1177/1087057109335743. Epub 2009 Jun 12. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Calmodulin acts as part of a calcium signal transduction pathway by mediating the control of a large number of enzymes, ion channels, aquaporins and other proteins through calcium-binding (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Calcium-binding is required for the activation of calmodulin (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Among the enzymes to be stimulated by the calmodulin-calcium complex are a number of protein kinases, such as myosin light-chain kinases and calmodulin-dependent protein kinase type II (CaMK2), and phosphatases (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis (PubMed:16760425). Is a regulator of voltage-dependent L-type calcium channels (PubMed:31454269). Mediates calcium-dependent inactivation of CACNA1C (PubMed:26969752). Positively regulates calcium-activated potassium channel activity of KCNN2 (PubMed:27165696). Forms a potassium channel complex with KCNQ1 and regulates electrophysiological activity of the channel via calcium-binding (PubMed:25441029). Acts as a sensor to modulate the endoplasmic reticulum contacts with other organelles mediated by VMP1:ATP2A2 (PubMed:28890335)
- Specific Function
- adenylate cyclase activator activity
Components:
Name | UniProt ID |
---|---|
Calmodulin-1 | P0DP23 |
Calmodulin-2 | P0DP24 |
Calmodulin-3 | P0DP25 |
References
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
Transporters
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- AcrA-AcrB-AcrZ-TolC is a drug efflux protein complex with broad substrate specificity that uses the proton motive force to export substrates.
- Specific Function
- efflux transmembrane transporter activity
- Gene Name
- acrB
- Uniprot ID
- P31224
- Uniprot Name
- Multidrug efflux pump subunit AcrB
- Molecular Weight
- 113572.75 Da
References
- Bailly C: Medicinal applications and molecular targets of dequalinium chloride. Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10. [Article]
- Yu EW, Aires JR, McDermott G, Nikaido H: A periplasmic drug-binding site of the AcrB multidrug efflux pump: a crystallographic and site-directed mutagenesis study. J Bacteriol. 2005 Oct;187(19):6804-15. doi: 10.1128/JB.187.19.6804-6815.2005. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 29, 2024 18:05