Explore a selection of our essential drug information below, or:
Identification
- Summary
Chlortetracycline is the first tetracycline antibiotic most commonly used for veterinary purposes.
- Generic Name
- Chlortetracycline
- DrugBank Accession Number
- DB09093
- Background
Chlortetracycline is a tetracycline antibiotic, and historically the first member of this class to be identified. It was discovered in 1945 by the scientist, Benjamin Minge Duggar, working at Lederle Laboratories under the supervision of Yellapragada Subbarow. He discovered that this antibiotic was the product of an actinomycete strain he cultured and obtained from a soil sample from a field in Missouri. The organism was named Streptomyces aureofaciens due to its gold-hued color.
- Type
- Small Molecule
- Groups
- Approved, Investigational, Vet approved
- Structure
Structure for Chlortetracycline (DB09093)
- Weight
- Average: 478.88
Monoisotopic: 478.114293429 - Chemical Formula
- C22H23ClN2O8
- Synonyms
- Chlortetracycline
- Chlortétracycline
- Chlortetracyclinum
- Clortetraciclina
Pharmacology
- Indication
Used in the manufacuring of medicated animal feeds Label.
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 Eye and eyelid infections •••••••••••• •••••••• • ••••• Treatment of Pyoderma •••••••••••• •••••••• Used in combination to treat Wound infections Combination Product in combination with: Chloramphenicol (DB00446), Neomycin (DB00994) ••• ••• •••••••• Used in combination to treat Corticosteroid-responsive dermatoses Combination Product in combination with: Triamcinolone (DB00620) •••••••••••• •••••• •••••••• ••••• - Contraindications & Blackbox Warnings
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Tetracycline antibiotics are bacteriostatic agents which act to inhibit bacterial growth and reproduction 2.
- Mechanism of action
Chlortetracycline, like other tetracyclines, competes for the A site of the bacterial ribosome 2. This binding competes with tRNA carrying amino acids preventing the addition of more amino acids to the peptide chain. This inhibition of protein synthesis ultimately inhibits growth and reproduction of the bacterial cell as necessary proteins cannot be synthesized.
Target Actions Organism A16S ribosomal RNA inhibitorEnteric bacteria and other eubacteria A30S ribosomal protein S3 inhibitorEscherichia coli (strain K12) A30S ribosomal protein S8 inhibitorEscherichia coli (strain K12) A30S ribosomal protein S19 inhibitorEscherichia coli (strain K12) A30S ribosomal protein S14 inhibitorEscherichia coli (strain K12) A30S ribosomal protein S7 inhibitorEscherichia coli (strain K12) UADP-ribosylation factor 1 inhibitorHumans UCatalase inhibitorMicrococcus luteus UEphrin type-B receptor 1 inhibitorHumans UPancreatic triacylglycerol lipase inhibitorHumans UProtein-arginine deiminase type-4 inhibitorHumans - Absorption
Chortetracycline reaches peak plasma concentation in about 3 hours 1. Its oral bioavailability is 25-30%.
- Volume of distribution
Chlortetracycline has a volume of distribution of 100 liters 1.
- Protein binding
Chlortetracline is 50-55% bound to plasma proteins 1.
- Metabolism
Chlortetracycline is not known to undergo significant metabolism 1.
- Route of elimination
Chlortetracycline is mainly eliminated in feces 1. Renal function does not appear to affect the rate of elimination.
- Half-life
The half-life of Chlortetracycline is 5.6 hours 1.
- Clearance
Not Available
- Adverse Effects
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The acute oral LD50 in mice is 2314mg/kg MSDS.The most common adverse effects of tertacylines are gastrointestinal disturbances, and staining of teeth and bone. Some occurences of dental hypoplasia and bone deformity have been noted 2. In pregnant women tetracyclines may produce hepatotoxicity.
- 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 softwareAcetylcysteine The therapeutic efficacy of Acetylcysteine can be decreased when used in combination with Chlortetracycline. Ambroxol The risk or severity of methemoglobinemia can be increased when Chlortetracycline is combined with Ambroxol. Articaine The risk or severity of methemoglobinemia can be increased when Chlortetracycline is combined with Articaine. Benzocaine The risk or severity of methemoglobinemia can be increased when Chlortetracycline is combined with Benzocaine. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Chlortetracycline 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 Chlortetracycline bisulfate 1D06KZ672I 27823-62-7 GQUMQTDURIYYIA-MRFRVZCGSA-N Chlortetracycline calcium complex NR4B2SX17S 57122-99-3 BRXWPGYMDYZZNU-NAUDNZITSA-L Chlortetracycline hydrochloride O1GX33ON8R 64-72-2 CBHYYLPALVVVEY-MRFRVZCGSA-N - International/Other Brands
- Aueromycin
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aureomycin - Ont Top 3% Ointment 3 % Topical Wyeth Ayerst Canada Inc. 1997-10-24 2000-08-02 Canada 
Aureomycin Ont 3% Ointment 3 % Topical Lederle Cyanamid Canada Inc. 1952-12-31 1997-11-24 Canada Aureomycin Ont Oph 1% Ointment 1 % Ophthalmic Lederle Cyanamid Canada Inc. 1955-12-31 1997-01-14 Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image ขี้ผึ้งทรามัยซิน ใส่แผล Ointment 3 %w/w Topical บริษัท แลชแมน จำกัด จำกัด 1986-01-16 Not applicable Thailand 
ขี้ผึ้งใส่แผล ฮีโร่มัยซิน Ointment 3 %w/w Topical บริษัท ฮีโร่มัยซิน ฟาร์ม่า จำกัด จำกัด 2003-04-23 Not applicable Thailand ออริโอมัยซิน * Ointment 3 %w/w Topical บริษัท อินเตอร์ไทย ฟาร์มาซูติเคิ้ล แมนูแฟคเจอริ่ง จำกัด จำกัด 1998-01-30 Not applicable Thailand โคบาล มัยซิน ออยเม้นท์ Ointment 3 %w/w Topical บริษัท ไบร์วู๊ดฟาร์มาซูติคอล จำกัด 1987-08-03 Not applicable Thailand - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Aureocort 1 mg/g + 30 mg/g Salbe Chlortetracycline hydrochloride (30 mg/g) + Triamcinolone acetonide (1 mg/g) Ointment Topical Dermapharm Gmb H 1966-09-28 Not applicable Austria 
ไทรไมซิน ออยท์เมนท์ Chlortetracycline (5 MG/1G) + Chloramphenicol (5 MG/1G) + Neomycin (5 MG/1G) Ointment Topical บริษัท สหแพทย์เภสัช จำกัด 2017-01-25 2020-08-24 Thailand
Categories
- ATC Codes
- D06AA02 — Chlortetracycline
- D06AA — Tetracycline and derivatives
- D06A — ANTIBIOTICS FOR TOPICAL USE
- D06 — ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE
- D — DERMATOLOGICALS
- J01AA — Tetracyclines
- J01A — TETRACYCLINES
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J01AA — Tetracyclines
- J01A — TETRACYCLINES
- J01 — ANTIBACTERIALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Agents that produce neuromuscular block (indirect)
- Alimentary Tract and Metabolism
- Anti-Bacterial Agents
- Anti-Infective Agents
- Antibacterials for Systemic Use
- Antibiotics for Topical Use
- Antiinfectives and Antiseptics for Local Oral Treatment
- Antiinfectives for Systemic Use
- Antiparasitic Agents
- Antiprotozoals
- Dermatologicals
- Enzyme Inhibitors
- Naphthacenes
- Ophthalmologicals
- Protein Synthesis Inhibitors
- Sensory Organs
- Stomatological Preparations
- Tetracyclines
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as tetracyclines. These are polyketides having an octahydrotetracene-2-carboxamide skeleton, substituted with many hydroxy and other groups.
- Kingdom
- Organic compounds
- Super Class
- Phenylpropanoids and polyketides
- Class
- Tetracyclines
- Sub Class
- Not Available
- Direct Parent
- Tetracyclines
- Alternative Parents
- Naphthacenes / Anthracenecarboxylic acids and derivatives / Tetralins / Aryl ketones / 1-hydroxy-2-unsubstituted benzenoids / Aralkylamines / Cyclohexenones / Aryl chlorides / Vinylogous acids / Tertiary alcohols show 9 more
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / Alcohol / Amine / Amino acid or derivatives / Anthracene carboxylic acid or derivatives / Aralkylamine / Aromatic homopolycyclic compound / Aryl chloride / Aryl halide / Aryl ketone show 26 more
- Molecular Framework
- Aromatic homopolycyclic compounds
- External Descriptors
- tertiary alcohol, tertiary amino compound, monocarboxylic acid amide, monochlorobenzenes, tetracyclines (CHEBI:27644) / Linear tetracyclines (C06571) / Linear tetracyclines (LMPK07000004)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- WCK1KIQ23Q
- CAS number
- 57-62-5
- InChI Key
- CYDMQBQPVICBEU-XRNKAMNCSA-N
- InChI
- InChI=1S/C22H23ClN2O8/c1-21(32)7-6-8-15(25(2)3)17(28)13(20(24)31)19(30)22(8,33)18(29)11(7)16(27)12-10(26)5-4-9(23)14(12)21/h4-5,7-8,15,26,28-29,32-33H,6H2,1-3H3,(H2,24,31)/t7-,8-,15-,21-,22-/m0/s1
- IUPAC Name
- (4S,4aS,5aS,6S,12aS)-7-chloro-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
- SMILES
- [H][C@@]12C[C@@]3([H])C(=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@H]2N(C)C)C(=O)C1=C(O)C=CC(Cl)=C1[C@@]3(C)O
References
- General References
- Agwuh KN, MacGowan A: Pharmacokinetics and pharmacodynamics of the tetracyclines including glycylcyclines. J Antimicrob Chemother. 2006 Aug;58(2):256-65. Epub 2006 Jul 1. [Article]
- 49, 50. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 614, 629). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- External Links
- KEGG Drug
- D07689
- KEGG Compound
- C06571
- PubChem Compound
- 54708735
- PubChem Substance
- 310265020
- ChemSpider
- 10469370
- 2408
- ChEBI
- 27644
- ChEMBL
- CHEMBL404520
- ZINC
- ZINC000019701769
- PDBe Ligand
- CTC
- Wikipedia
- Chlortetracycline
- PDB Entries
- 2fj1 / 2tct / 2y6r / 3egz / 4v2g / 5tui / 6qjw / 6umw
- FDA label
- Download (218 KB)
- MSDS
- Download (179 KB)
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 data0 Terminated Treatment Osteomyelitis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Cream Capsule Topical 250 MG Cream Ophthalmic 1 % Ointment Topical 3 % Solution / drops 20 ML Ointment Ophthalmic 1 % Ointment Ophthalmic 10 mg/g Ointment Topical 3 %w/w Capsule 250 mg Ointment Topical - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) Decomposes at 210-215 MSDS - Predicted Properties
Property Value Source Water Solubility 0.259 mg/mL ALOGPS logP -0.13 ALOGPS logP -2.9 Chemaxon logS -3.3 ALOGPS pKa (Strongest Acidic) 2.99 Chemaxon pKa (Strongest Basic) 9.04 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 9 Chemaxon Hydrogen Donor Count 6 Chemaxon Polar Surface Area 181.62 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 118.99 m3·mol-1 Chemaxon Polarizability 45.61 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-01t9-0000900000-a3bd564bfed5c6bc761b Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-002f-0009700000-c725c9e77c980b61f11f Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0000900000-0823696773829952578f Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-0009400000-53a084c65f0be98ed440 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-03xr-3695300000-c8973e90dc33f7f8d08d Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-08gi-2019500000-9eb19da0c650341d3d22 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]- 212.5838107 predictedDarkChem Lite v0.1.0 [M-H]- 205.57065 predictedDeepCCS 1.0 (2019) [M+H]+ 211.6348107 predictedDarkChem Lite v0.1.0 [M+H]+ 207.46608 predictedDeepCCS 1.0 (2019) [M+Na]+ 210.4818107 predictedDarkChem Lite v0.1.0 [M+Na]+ 213.27031 predictedDeepCCS 1.0 (2019)
Targets
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Yes
Inhibitor
References
- Nawaz M, Sung K, Khan SA, Khan AA, Steele R: Biochemical and molecular characterization of tetracycline-resistant Aeromonas veronii isolates from catfish. Appl Environ Microbiol. 2006 Oct;72(10):6461-6. [Article]
- Domingue GJ Sr: Cryptic bacterial infection in chronic prostatitis: diagnostic and therapeutic implications. Curr Opin Urol. 1998 Jan;8(1):45-9. [Article]
- Pringle M, Fellstrom C, Johansson KE: Decreased susceptibility to doxycycline associated with a 16S rRNA gene mutation in Brachyspira hyodysenteriae. Vet Microbiol. 2007 Jul 20;123(1-3):245-8. Epub 2007 Feb 25. [Article]
- Rasmussen B, Noller HF, Daubresse G, Oliva B, Misulovin Z, Rothstein DM, Ellestad GA, Gluzman Y, Tally FP, Chopra I: Molecular basis of tetracycline action: identification of analogs whose primary target is not the bacterial ribosome. Antimicrob Agents Chemother. 1991 Nov;35(11):2306-11. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Binds the lower part of the 30S subunit head. Binds mRNA in the 70S ribosome, positioning it for translation (By similarity).
- Specific Function
- mRNA binding
- Gene Name
- rpsC
- Uniprot ID
- P0A7V3
- Uniprot Name
- 30S ribosomal protein S3
- Molecular Weight
- 25983.07 Da
References
- Buck MA, Cooperman BS: Single protein omission reconstitution studies of tetracycline binding to the 30S subunit of Escherichia coli ribosomes. Biochemistry. 1990 Jun 5;29(22):5374-9. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- One of the primary rRNA binding proteins, it binds directly to 16S rRNA central domain where it helps coordinate assembly of the platform of the 30S subunit.
- Specific Function
- rRNA binding
- Gene Name
- rpsH
- Uniprot ID
- P0A7W7
- Uniprot Name
- 30S ribosomal protein S8
- Molecular Weight
- 14126.435 Da
References
- Buck MA, Cooperman BS: Single protein omission reconstitution studies of tetracycline binding to the 30S subunit of Escherichia coli ribosomes. Biochemistry. 1990 Jun 5;29(22):5374-9. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- In the E.coli 70S ribosome in the initiation state (PubMed:12809609) it has been modeled to contact the 23S rRNA of the 50S subunit forming part of bridge B1a; this bridge is broken in the model with bound EF-G. The 23S rRNA contact site in bridge B1a is modeled to differ in different ribosomal states (PubMed:12859903), contacting alternately S13 or S19. In the 3.5 angstroms resolved ribosome structures (PubMed:16272117) the contacts between L5, S13 and S19 bridge B1b are different, confirming the dynamic nature of this interaction. Bridge B1a is not visible in the crystallized ribosomes due to 23S rRNA disorder.
- Specific Function
- rRNA binding
- Gene Name
- rpsS
- Uniprot ID
- P0A7U3
- Uniprot Name
- 30S ribosomal protein S19
- Molecular Weight
- 10430.235 Da
References
- Buck MA, Cooperman BS: Single protein omission reconstitution studies of tetracycline binding to the 30S subunit of Escherichia coli ribosomes. Biochemistry. 1990 Jun 5;29(22):5374-9. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Binds 16S rRNA, required for the assembly of 30S particles and may also be responsible for determining the conformation of the 16S rRNA at the A site.
- Specific Function
- rRNA binding
- Gene Name
- rpsN
- Uniprot ID
- P0AG59
- Uniprot Name
- 30S ribosomal protein S14
- Molecular Weight
- 11580.36 Da
References
- Buck MA, Cooperman BS: Single protein omission reconstitution studies of tetracycline binding to the 30S subunit of Escherichia coli ribosomes. Biochemistry. 1990 Jun 5;29(22):5374-9. [Article]
- Kind
- Protein
- Organism
- Escherichia coli (strain K12)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- One of the primary rRNA binding proteins, it binds directly to 16S rRNA where it nucleates assembly of the head domain of the 30S subunit (PubMed:2461734). Is located at the subunit interface close to the decoding center, where it has been shown to contact mRNA (PubMed:10606263). Has been shown to contact tRNA in both the P and E sites; it probably blocks exit of the E site tRNA (PubMed:8524654).
- Specific Function
- mRNA binding
- Gene Name
- rpsG
- Uniprot ID
- P02359
- Uniprot Name
- 30S ribosomal protein S7
- Molecular Weight
- 20018.91 Da
References
- Buck MA, Cooperman BS: Single protein omission reconstitution studies of tetracycline binding to the 30S subunit of Escherichia coli ribosomes. Biochemistry. 1990 Jun 5;29(22):5374-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Small GTPase involved in protein trafficking between different compartments (PubMed:8253837). Modulates vesicle budding and uncoating within the Golgi complex (PubMed:8253837). In its GTP-bound form, triggers the recruitment of coatomer proteins to the Golgi membrane (PubMed:8253837). The hydrolysis of ARF1-bound GTP, which is mediated by ARFGAPs proteins, is required for dissociation of coat proteins from Golgi membranes and vesicles (PubMed:8253837). The GTP-bound form interacts with PICK1 to limit PICK1-mediated inhibition of Arp2/3 complex activity; the function is linked to AMPA receptor (AMPAR) trafficking, regulation of synaptic plasticity of excitatory synapses and spine shrinkage during long-term depression (LTD) (By similarity). Plays a key role in the regulation of intestinal stem cells and gut microbiota, and is essential for maintaining intestinal homeostasis (By similarity). Plays also a critical role in mast cell expansion but not in mast cell maturation by facilitating optimal mTORC1 activation (By similarity)
- Specific Function
- GTP binding
- Gene Name
- ARF1
- Uniprot ID
- P84077
- Uniprot Name
- ADP-ribosylation factor 1
- Molecular Weight
- 20696.62 Da
References
- Macia E, Vazquez-Rojas M, Robiolo A, Fayad R, Abelanet S, Mus-Veteau I, Fontaine-Vive F, Mehiri M, Luton F, Franco M: Chlortetracycline, a Novel Arf Inhibitor That Decreases the Arf6-Dependent Invasive Properties of Breast Cancer Cells. Molecules. 2021 Feb 12;26(4). pii: molecules26040969. doi: 10.3390/molecules26040969. [Article]
- Kind
- Protein
- Organism
- Micrococcus luteus
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Decomposes hydrogen peroxide into water and oxygen; serves to protect cells from the toxic effects of hydrogen peroxide.
- Specific Function
- catalase activity
- Gene Name
- katA
- Uniprot ID
- P29422
- Uniprot Name
- Catalase
- Molecular Weight
- 56905.52 Da
References
- Ren L, Wang Q, Du Y, Xu P, Zong W: Research on the Impact and Mechanism for the Inhibition of Micrococcus Catalase Activity by Typical Tetracyclines. Biomed Res Int. 2020 Oct 13;2020:5085369. doi: 10.1155/2020/5085369. eCollection 2020. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Cognate/functional ephrin ligands for this receptor include EFNB1, EFNB2 and EFNB3. During nervous system development, regulates retinal axon guidance redirecting ipsilaterally ventrotemporal retinal ganglion cells axons at the optic chiasm midline. This probably requires repulsive interaction with EFNB2. In the adult nervous system together with EFNB3, regulates chemotaxis, proliferation and polarity of the hippocampus neural progenitors. In addition to its role in axon guidance also plays an important redundant role with other ephrin-B receptors in development and maturation of dendritic spines and synapse formation. May also regulate angiogenesis. More generally, may play a role in targeted cell migration and adhesion. Upon activation by EFNB1 and probably other ephrin-B ligands activates the MAPK/ERK and the JNK signaling cascades to regulate cell migration and adhesion respectively. Involved in the maintenance of the pool of satellite cells (muscle stem cells) by promoting their self-renewal and reducing their activation and differentiation (By similarity)
- Specific Function
- ATP binding
- Gene Name
- EPHB1
- Uniprot ID
- P54762
- Uniprot Name
- Ephrin type-B receptor 1
- Molecular Weight
- 109884.175 Da
References
- Ahmed MS, Wang P, Nguyen NUN, Nakada Y, Menendez-Montes I, Ismail M, Bachoo R, Henkemeyer M, Sadek HA, Kandil ES: Identification of tetracycline combinations as EphB1 tyrosine kinase inhibitors for treatment of neuropathic pain. Proc Natl Acad Sci U S A. 2021 Mar 9;118(10). pii: 2016265118. doi: 10.1073/pnas.2016265118. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Plays an important role in fat metabolism. It preferentially splits the esters of long-chain fatty acids at positions 1 and 3, producing mainly 2-monoacylglycerol and free fatty acids, and shows considerably higher activity against insoluble emulsified substrates than against soluble ones
- Specific Function
- all-trans-retinyl-palmitate hydrolase, all-trans-retinol forming activity
- Gene Name
- PNLIP
- Uniprot ID
- P16233
- Uniprot Name
- Pancreatic triacylglycerol lipase
- Molecular Weight
- 51156.48 Da
References
- ROKOS J, MALEK P, BURGER M, PROCHAZKA P, KOLC J: The effect of divalent metals on the inhibition of pancreatic lipase by chlortetracycline. Antibiot Chemother (Northfield). 1959 Oct;9:600-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Catalyzes the citrullination/deimination of arginine residues of proteins such as histones, thereby playing a key role in histone code and regulation of stem cell maintenance (PubMed:15339660, PubMed:15345777, PubMed:16567635, PubMed:21245532). Citrullinates histone H1 at 'Arg-54' (to form H1R54ci), histone H3 at 'Arg-2', 'Arg-8', 'Arg-17' and/or 'Arg-26' (to form H3R2ci, H3R8ci, H3R17ci, H3R26ci, respectively) and histone H4 at 'Arg-3' (to form H4R3ci) (PubMed:15339660, PubMed:15345777, PubMed:16567635, PubMed:21245532). Acts as a key regulator of stem cell maintenance by mediating citrullination of histone H1: citrullination of 'Arg-54' of histone H1 (H1R54ci) results in H1 displacement from chromatin and global chromatin decondensation, thereby promoting pluripotency and stem cell maintenance (PubMed:15339660, PubMed:15345777, PubMed:16567635, PubMed:21245532). Promotes profound chromatin decondensation during the innate immune response to infection in neutrophils by mediating formation of H1R54ci (PubMed:18209087). Required for the formation of neutrophil extracellular traps (NETs); NETs are mainly composed of DNA fibers and are released by neutrophils to bind pathogens during inflammation (By similarity). Citrullination of histone H3 prevents their methylation by CARM1 and HRMT1L2/PRMT1 and represses transcription (PubMed:15345777). Citrullinates EP300/P300 at 'Arg-2142', which favors its interaction with NCOA2/GRIP1 (PubMed:15731352)
- Specific Function
- calcium ion binding
- Gene Name
- PADI4
- Uniprot ID
- Q9UM07
- Uniprot Name
- Protein-arginine deiminase type-4
- Molecular Weight
- 74078.65 Da
References
- Knuckley B, Luo Y, Thompson PR: Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors. Bioorg Med Chem. 2008 Jan 15;16(2):739-45. Epub 2007 Oct 13. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Bratlid D, Bergan T: Displacement of albumin-bound antimicrobial agents by bilirubin. Pharmacology. 1976;14(5):464-72. doi: 10.1159/000136629. [Article]
Drug created at September 16, 2015 17:03 / Updated at October 07, 2024 17:58