Antithymocyte immunoglobulin (rabbit)
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Identification
- Summary
Antithymocyte immunoglobulin (rabbit) is a purified form of rabbit anti-thymocyte antibodies used for immunosuppression in patients receiving kidney transplants.
- Generic Name
- Antithymocyte immunoglobulin (rabbit)
- DrugBank Accession Number
- DB00098
- Background
Rabbit anti-thymocyte globulin. Thymoglobulin is a polyclonal antibody that suppresses certain types of immune cells responsible for acute organ rejection in transplant patients. Thymoglobulin is a mixture of antibodies intended to bind to various cell surface antigens. The most common mode of action of Thymoglobulin is via selective depletion of T-cells.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Polyclonal antibody (pAb) - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- Anti-human thymocyte immunoglobulin, rabbit
- Anti-T-lymphocyte immune globulin, rabbit
- Anti-thymocyte globulin (rabbit)
- Anti-thymocyte globulin rabbit
- Antithymocyte immunoglobulin
- Lapine T-lymphocyte immune globulin
- Rabbit anti-human thymocyte globulin
- Rabbit anti-human thymocyte globulin (rATG)
- Rabbit anti-human thymocyte immunoglobulin
- Rabbit anti-thymocyte immunoglobulin
- Rabbit antithymocyte globulin
- Rabbit ATG
- rATG
- Thymoglobulin
- Thymoglobuline
Pharmacology
- Indication
For prevention of renal transplant rejection
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 Adjunct therapy in prophylaxis of Rejection acute renal •••••••••••• ••••••••• Adjunct therapy in management of Rejection acute renal •••••••••••• ••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Antithymocyte Globulin (ATG) is a concentrated anti-human T-lymphocyte immunoglobulin preparation derived from rabbits after immunization with a T-lympoblast cell line. ATG is an immunosuppressive product for the prevention and treatment of acute rejection following organ transplantation. ATG reduces the host immune response against tissue transplants or organ allografts.
- Mechanism of action
Binds to multiple, T-cell specific antigens leading to T-lymphocyte cell death via complement mediated cytotoxicity or apoptosis.
Target Actions Organism AMajor histocompatibility complex class I-related gene protein antagonistHumans AIntegrin alpha-L Not Available Humans AT-lymphocyte activation antigen CD86 binderHumans ALow affinity immunoglobulin gamma Fc region receptor II-b Not Available Humans AT-cell surface glycoprotein CD4 Not Available Humans AIntegrin beta-1 Not Available Humans AIntegrin alpha-V Not Available Humans AIntegrin beta-3 Not Available Humans UT-cell surface glycoprotein CD1a inhibitorHumans - Absorption
T-cell depletion usually observed within 1 day after initiating therapy. Average 21.5 and 87 mcg/mL 4–8 hours post-infusion after first and last IV doses, respectively, when given for 7–11 days.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Most likely removed by opsonization via the reticuloendothelial system when bound to T lymphocytes, or by human antimurine antibody production.
- Route of elimination
Not Available
- Half-life
2-3 days, may increase after multiple doses administration
- Clearance
Not 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
Not known whether ATG (rabbit) distributes into human milk; however, other immunoglobulins are distributed into human milk.
- 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 softwareAbatacept The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Antithymocyte immunoglobulin (rabbit). Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Antithymocyte immunoglobulin (rabbit). Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Antithymocyte immunoglobulin (rabbit). Aducanumab The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Aducanumab. - 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.
- International/Other Brands
- ATG-Fresenius (Fresenius SE) / ATG-Fresenius S (Fresenius SE)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Thymoglobulin Injection, powder, lyophilized, for solution 5 mg/1mL Intravenous Genzyme Corporation 1998-12-30 Not applicable US Thymoglobulin Powder, for solution 25 mg / vial Intravenous Sanofi Aventis Deutschland Gmb H 2003-05-06 Not applicable Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image GRAFALON 5 ML IV INFUZYONLUK COZELTI KONSANTRESI ICEREN FLAKON, 1 ADET Antithymocyte immunoglobulin (rabbit) (5 ml) Injection, solution Intravenous FRESENIUS MEDİKAL HİZMETLER A.Ş. 2016-03-15 Not applicable Turkey
Categories
- ATC Codes
- L04AA04 — Antithymocyte immunoglobulin (rabbit)
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibody-Surface Protein Interactions
- Antineoplastic and Immunomodulating Agents
- Biological Products
- Blood
- Blood Proteins
- Body Fluids
- Complex Mixtures
- Fluids and Secretions
- Globulins
- Immune Sera
- Immunoglobulin G
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Immunotherapy
- Increased T Lymphocyte Destruction
- Lymphocyte Function Alteration
- Miscellaneous Therapeutic Agents
- Proteins
- Selective Immunosuppressants
- Serum
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- D7RD81HE4W
- CAS number
- 308067-60-9
References
- General References
- FDA Approved Drug Products: THYMOGLOBULIN (anti-thymocyte globulin [rabbit]) for intravenous use [Link]
- External Links
- PubChem Substance
- 46506920
- 107044
- Therapeutic Targets Database
- DAP001300
- PharmGKB
- PA164743704
- Wikipedia
- Anti-thymocyte_globulin
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 Active Not Recruiting Other Severe Aplastic Anemia (SAA) 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Allografts / Lung Transplant 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Aplastic Anemia / Dyskeratosis Congenita 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Haemoglobinopathies congenital / Sickle Cell Disease (SCD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Acute Lymphocytic Leukemia (ALL) / Acute Myeloid Leukemia / Graft-versus-host Disease (GVHD) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Genzyme Inc.
- Dosage Forms
Form Route Strength Injection, solution, concentrate Intravenous 20 MG/ML Solution Intravenous 20 mg/ml Injection, solution, concentrate Intravenous Injection, solution Intravenous 5 ml Injection, powder, lyophilized, for solution Intravenous 5 mg/1mL Powder, for solution Intravenous 25 mg / vial Powder, for solution Intravenous 5 MG/ML Powder, for solution Parenteral 25 MG/5ML Injection Intravenous 5 mg/mL Injection, powder, lyophilized, for solution Parenteral Injection, powder, lyophilized, for solution Intravenous Injection, powder, for solution Intravenous 25 mg Solution Intravenous 25.000 mg Injection, powder, lyophilized, for solution Intravenous 25 mg Injection, powder, lyophilized, for solution Intravenous 2500000 mg Powder 5 mg/mL - Prices
Unit description Cost Unit Thymoglobulin 25 mg vial 636.48USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 61 °C (FAB fragment), 71 °C (whole mAb) Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Antigen-presenting molecule specialized in displaying microbial pyrimidine-based metabolites to alpha-beta T cell receptors (TCR) on innate-type mucosal-associated invariant T (MAIT) cells (PubMed:12794138, PubMed:19416870, PubMed:22692454, PubMed:23051753, PubMed:23846752, PubMed:26795251). In complex with B2M preferentially presents riboflavin-derived metabolites to semi-invariant TRAV1-2 TCRs on MAIT cells, guiding immune surveillance of the microbial metabolome at mucosal epithelial barriers (PubMed:20581831, PubMed:24695216, PubMed:26795251). Signature pyrimidine-based microbial antigens are generated via non-enzymatic condensation of metabolite intermediates of the riboflavin pathway with by-products arising from other metabolic pathways such as glycolysis. Typical potent antigenic metabolites are 5-(2-oxoethylideneamino)-6-D-ribitylaminouracil (5-OE-RU) and 5-(2-oxopropylideneamino)-6-D-ribitylaminouracil (5-OP-RU), products of condensation of 5-amino-6-D-ribityaminouracil (5-A-RU) with glyoxal or methylglyoxal by-products, respectively (PubMed:24695216). May present microbial antigens to various TRAV1-2-negative MAIT cell subsets, providing for unique recognition of diverse microbes, including pathogens that do not synthesize riboflavin (PubMed:27527800, PubMed:31113973). Upon antigen recognition, elicits rapid innate-type MAIT cell activation to eliminate pathogenic microbes by directly killing infected cells (PubMed:23846752, PubMed:24695216, PubMed:27527800). During T cell development, drives thymic selection and post-thymic terminal differentiation of MAIT cells in a process dependent on commensal microflora (By similarity). Acts as an immune sensor of cancer cell metabolome (PubMed:31959982). May present a tumor-specific or -associated metabolite essential for cancer cell survival to a pan-cancer TCR consisting of TRAV38.2-DV8*TRAJ31 alpha chain paired with a TRBV25.1*TRBJ2.3 beta chain on a non-MAIT CD8-positive T cell clone (MC.7.G5), triggering T cell-mediated killing of a wide range of cancer cell types (PubMed:31959982)
- Specific Function
- beta-2-microglobulin binding
- Gene Name
- MR1
- Uniprot ID
- Q95460
- Uniprot Name
- Major histocompatibility complex class I-related gene protein
- Molecular Weight
- 39365.76 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Integrin ITGAL/ITGB2 is a receptor for ICAM1, ICAM2, ICAM3 and ICAM4. Integrin ITGAL/ITGB2 is a receptor for F11R (PubMed:11812992, PubMed:15528364). Integrin ITGAL/ITGB2 is a receptor for the secreted form of ubiquitin-like protein ISG15; the interaction is mediated by ITGAL (PubMed:29100055). Involved in a variety of immune phenomena including leukocyte-endothelial cell interaction, cytotoxic T-cell mediated killing, and antibody dependent killing by granulocytes and monocytes. Contributes to natural killer cell cytotoxicity (PubMed:15356110). Involved in leukocyte adhesion and transmigration of leukocytes including T-cells and neutrophils (PubMed:11812992). Required for generation of common lymphoid progenitor cells in bone marrow, indicating a role in lymphopoiesis (By similarity). Integrin ITGAL/ITGB2 in association with ICAM3, contributes to apoptotic neutrophil phagocytosis by macrophages (PubMed:23775590)
- Specific Function
- cell adhesion molecule binding
- Gene Name
- ITGAL
- Uniprot ID
- P20701
- Uniprot Name
- Integrin alpha-L
- Molecular Weight
- 128768.495 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Receptor involved in the costimulatory signal essential for T-lymphocyte proliferation and interleukin-2 production, by binding CD28 or CTLA-4 (PubMed:12196291). May play a critical role in the early events of T-cell activation and costimulation of naive T-cells, such as deciding between immunity and anergy that is made by T-cells within 24 hours after activation (PubMed:7527824). Also involved in the regulation of B cells function, plays a role in regulating the level of IgG(1) produced. Upon CD40 engagement, activates NF-kappa-B signaling pathway via phospholipase C and protein kinase C activation (By similarity)
- Specific Function
- coreceptor activity
- Gene Name
- CD86
- Uniprot ID
- P42081
- Uniprot Name
- T-lymphocyte activation antigen CD86
- Molecular Weight
- 37681.97 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Binding to this receptor results in down-modulation of previous state of cell activation triggered via antigen receptors on B-cells (BCR), T-cells (TCR) or via another Fc receptor. Isoform IIB1 fails to mediate endocytosis or phagocytosis. Isoform IIB2 does not trigger phagocytosis
- Specific Function
- amyloid-beta binding
- Gene Name
- FCGR2B
- Uniprot ID
- P31994
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor II-b
- Molecular Weight
- 34043.355 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Integral membrane glycoprotein that plays an essential role in the immune response and serves multiple functions in responses against both external and internal offenses. In T-cells, functions primarily as a coreceptor for MHC class II molecule:peptide complex. The antigens presented by class II peptides are derived from extracellular proteins while class I peptides are derived from cytosolic proteins. Interacts simultaneously with the T-cell receptor (TCR) and the MHC class II presented by antigen presenting cells (APCs). In turn, recruits the Src kinase LCK to the vicinity of the TCR-CD3 complex. LCK then initiates different intracellular signaling pathways by phosphorylating various substrates ultimately leading to lymphokine production, motility, adhesion and activation of T-helper cells. In other cells such as macrophages or NK cells, plays a role in differentiation/activation, cytokine expression and cell migration in a TCR/LCK-independent pathway. Participates in the development of T-helper cells in the thymus and triggers the differentiation of monocytes into functional mature macrophages
- Specific Function
- coreceptor activity
- Gene Name
- CD4
- Uniprot ID
- P01730
- Uniprot Name
- T-cell surface glycoprotein CD4
- Molecular Weight
- 51110.205 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are receptors for collagen. Integrins alpha-1/beta-1 and alpha-2/beta-2 recognize the proline-hydroxylated sequence G-F-P-G-E-R in collagen. Integrins alpha-2/beta-1, alpha-3/beta-1, alpha-4/beta-1, alpha-5/beta-1, alpha-8/beta-1, alpha-10/beta-1, alpha-11/beta-1 and alpha-V/beta-1 are receptors for fibronectin. Alpha-4/beta-1 recognizes one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. Integrin alpha-5/beta-1 is a receptor for fibrinogen. Integrin alpha-1/beta-1, alpha-2/beta-1, alpha-6/beta-1 and alpha-7/beta-1 are receptors for lamimin. Integrin alpha-6/beta-1 (ITGA6:ITGB1) is present in oocytes and is involved in sperm-egg fusion (By similarity). Integrin alpha-4/beta-1 is a receptor for VCAM1. It recognizes the sequence Q-I-D-S in VCAM1. Integrin alpha-9/beta-1 is a receptor for VCAM1, cytotactin and osteopontin. It recognizes the sequence A-E-I-D-G-I-E-L in cytotactin. Integrin alpha-3/beta-1 is a receptor for epiligrin, thrombospondin and CSPG4. Alpha-3/beta-1 may mediate with LGALS3 the stimulation by CSPG4 of endothelial cells migration. Integrin alpha-V/beta-1 is a receptor for vitronectin. Beta-1 integrins recognize the sequence R-G-D in a wide array of ligands. When associated with alpha-7 integrin, regulates cell adhesion and laminin matrix deposition. Involved in promoting endothelial cell motility and angiogenesis. Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process and the formation of mineralized bone nodules. May be involved in up-regulation of the activity of kinases such as PKC via binding to KRT1. Together with KRT1 and RACK1, serves as a platform for SRC activation or inactivation. Plays a mechanistic adhesive role during telophase, required for the successful completion of cytokinesis. Integrin alpha-3/beta-1 provides a docking site for FAP (seprase) at invadopodia plasma membranes in a collagen-dependent manner and hence may participate in the adhesion, formation of invadopodia and matrix degradation processes, promoting cell invasion. ITGA4:ITGB1 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGA4:ITGB1 and ITGA5:ITGB1 bind to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGA5:ITGB1 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887, PubMed:17158881). ITGA5:ITGB1 acts as a receptor for fibronectin FN1 and mediates R-G-D-dependent cell adhesion to FN1 (PubMed:33962943). ITGA5:ITGB1 is a receptor for IL1B and binding is essential for IL1B signaling (PubMed:29030430). ITGA5:ITGB3 is a receptor for soluble CD40LG and is required for CD40/CD40LG signaling (PubMed:31331973). Plays an important role in myoblast differentiation and fusion during skeletal myogenesis (By similarity). ITGA9:ITGB1 may play a crucial role in SVEP1/polydom-mediated myoblast cell adhesion (By similarity). Integrins ITGA9:ITGB1 and ITGA4:ITGB1 repress PRKCA-mediated L-type voltage-gated channel Ca(2+) influx and ROCK-mediated calcium sensitivity in vascular smooth muscle cells via their interaction with SVEP1, thereby inhibit vasocontraction (PubMed:35802072)
- Specific Function
- actin binding
- Gene Name
- ITGB1
- Uniprot ID
- P05556
- Uniprot Name
- Integrin beta-1
- Molecular Weight
- 88414.575 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fibrinogen, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin and vWF. They recognize the sequence R-G-D in a wide array of ligands. ITGAV:ITGB3 binds to fractalkine (CX3CL1) and may act as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 and ITGAV:ITGB6 act as receptors for fibrillin-1 (FBN1) and mediate R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887, PubMed:17158881). Integrin alpha-V/beta-6 or alpha-V/beta-8 (ITGAV:ITGB6 or ITGAV:ITGB8) mediates R-G-D-dependent release of transforming growth factor beta-1 (TGF-beta-1) from regulatory Latency-associated peptide (LAP), thereby playing a key role in TGF-beta-1 activation (PubMed:15184403, PubMed:22278742, PubMed:28117447). ITGAV:ITGB3 acts as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428)
- Specific Function
- coreceptor activity
- Gene Name
- ITGAV
- Uniprot ID
- P06756
- Uniprot Name
- Integrin alpha-V
- Molecular Weight
- 116036.855 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General Function
- Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha-V/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha-IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets (By similarity). ITGAV:ITGB3 binds to fractalkine (CX3CL1) and acts as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887). In brain, plays a role in synaptic transmission and plasticity. Involved in the regulation of the serotonin neurotransmission, is required to localize to specific compartments within the synapse the serotonin receptor SLC6A4 and for an appropriate reuptake of serotonin. Controls excitatory synaptic strength by regulating GRIA2-containing AMPAR endocytosis, which affects AMPAR abundance and composition (By similarity). ITGAV:ITGB3 act as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428)
- Specific Function
- cell adhesion molecule binding
- Gene Name
- ITGB3
- Uniprot ID
- P05106
- Uniprot Name
- Integrin beta-3
- Molecular Weight
- 87056.975 Da
References
- Monti P, Allavena P, Di Carlo V, Piemonti L: Effects of anti-lymphocytes and anti-thymocytes globulin on human dendritic cells. Int Immunopharmacol. 2003 Feb;3(2):189-96. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Antigen-presenting protein that binds self and non-self lipid and glycolipid antigens and presents them to T-cell receptors on natural killer T-cells
- Specific Function
- endogenous lipid antigen binding
- Gene Name
- CD1A
- Uniprot ID
- P06126
- Uniprot Name
- T-cell surface glycoprotein CD1a
- Molecular Weight
- 37077.1 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 29, 2024 14:47