Target Information
| Target General Information | Top | |||||
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| Target ID |
T07403
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| Target Name |
Integrin alpha-4/beta-7 (ITGA4/B7)
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| Synonyms |
alpha(4)beta(7) integrin; Alpha 4 beta 7 integrin
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| Gene Name |
ITGA4-ITGB7
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Crohn disease [ICD-11: DD70] | |||||
| Function |
It is expressed on lymphocytes and is responsible for T-cell homing into gut-associated lymphoid tissues through its binding to mucosal addressin cell adhesion molecule (MAdCAM), which is present on high endothelial venules of mucosal lymphoid organs.
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| BioChemical Class |
Integrin
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| UniProt ID | ||||||
| Sequence |
MVALPMVLVLLLVLSRGESELDAKIPSTGDATEWRNPHLSMLGSCQPAPSCQKCILSHPS
CAWCKQLNFTASGEAEARRCARREELLARGCPLEELEEPRGQQEVLQDQPLSQGARGEGA TQLAPQRVRVTLRPGEPQQLQVRFLRAEGYPVDLYYLMDLSYSMKDDLERVRQLGHALLV RLQEVTHSVRIGFGSFVDKTVLPFVSTVPSKLRHPCPTRLERCQSPFSFHHVLSLTGDAQ AFEREVGRQSVSGNLDSPEGGFDAILQAALCQEQIGWRNVSRLLVFTSDDTFHTAGDGKL GGIFMPSDGHCHLDSNGLYSRSTEFDYPSVGQVAQALSAANIQPIFAVTSAALPVYQELS KLIPKSAVGELSEDSSNVVQLIMDAYNSLSSTVTLEHSSLPPGVHISYESQCEGPEKREG KAEDRGQCNHVRINQTVTFWVSLQATHCLPEPHLLRLRALGFSEELIVELHTLCDCNCSD TQPQAPHCSDGQGHLQCGVCSCAPGRLGRLCECSVAELSSPDLESGCRAPNGTGPLCSGK GHCQCGRCSCSGQSSGHLCECDDASCERHEGILCGGFGRCQCGVCHCHANRTGRACECSG DMDSCISPEGGLCSGHGRCKCNRCQCLDGYYGALCDQCPGCKTPCERHRDCAECGAFRTG PLATNCSTACAHTNVTLALAPILDDGWCKERTLDNQLFFFLVEDDARGTVVLRVRPQEKG ADHTQAIVLGCVGGIVAVGLGLVLAYRLSVEIYDRREYSRFEKEQQQLNWKQDSNPLYKS AITTTINPRFQEADSPTLMAWEARREPGPRRAAVRETVMLLLCLGVPTGRPYNVDTESAL LYQGPHNTLFGYSVVLHSHGANRWLLVGAPTANWLANASVINPGAIYRCRIGKNPGQTCE QLQLGSPNGEPCGKTCLEERDNQWLGVTLSRQPGENGSIVTCGHRWKNIFYIKNENKLPT GGCYGVPPDLRTELSKRIAPCYQDYVKKFGENFASCQAGISSFYTKDLIVMGAPGSSYWT GSLFVYNITTNKYKAFLDKQNQVKFGSYLGYSVGAGHFRSQHTTEVVGGAPQHEQIGKAY IFSIDEKELNILHEMKGKKLGSYFGASVCAVDLNADGFSDLLVGAPMQSTIREEGRVFVY INSGSGAVMNAMETNLVGSDKYAARFGESIVNLGDIDNDGFEDVAIGAPQEDDLQGAIYI YNGRADGISSTFSQRIEGLQISKSLSMFGQSISGQIDADNNGYVDVAVGAFRSDSAVLLR TRPVVIVDASLSHPESVNRTKFDCVENGWPSVCIDLTLCFSYKGKEVPGYIVLFYNMSLD VNRKAESPPRFYFSSNGTSDVITGSIQVSSREANCRTHQAFMRKDVRDILTPIQIEAAYH LGPHVISKRSTEEFPPLQPILQQKKEKDIMKKTINFARFCAHENCSADLQVSAKIGFLKP HENKTYLAVGSMKTLMLNVSLFNAGDDAYETTLHVKLPVGLYFIKILELEEKQINCEVTD NSGVVQLDCSIGYIYVDHLSRIDISFLLDVSSLSRAEEDLSITVHATCENEEEMDNLKHS RVTVAIPLKYEVKLTVHGFVNPTSFVYGSNDENEPETCMVEKMNLTFHVINTGNSMAPNV SVEIMVPNSFSPQTDKLFNILDVQTTTGECHFENYQRVCALEQQKSAMQTLKGIVRFLSK TDKRLLYCIKADPHCLNFLCNFGKMESGKEASVHIQLEGRPSILEMDETSALKFEIRATG FPEPNPRVIELNKDENVAHVLLEGLHHQRPKRYFTIVIISSSLLLGLIVLLLISYVMWKA GFFKRQYKSILQEENRRDSWSYINSKSNDD Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | MLN0002 | Drug Info | Approved | Crohn disease | [1], [2], [3] | |
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | MORF-057 | Drug Info | Phase 2 | Crohn disease | [4] | |
| 2 | PN-943 | Drug Info | Phase 2 | Ulcerative colitis | [5] | |
| 3 | TRK-170 | Drug Info | Phase 2 | Inflammatory bowel disease | [6] | |
| 4 | GS-1427 | Drug Info | Phase 1 | Inflammatory bowel disease | [7] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | R1295 | Drug Info | Discontinued in Phase 1 | Rheumatoid arthritis | [8] | |
| 2 | TR-14035 | Drug Info | Discontinued in Phase 1 | Multiple sclerosis | [9] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | MLN0002 | Drug Info | [1] | |||
| 2 | TRK-170 | Drug Info | [11] | |||
| 3 | R1295 | Drug Info | [12] | |||
| 4 | TR-14035 | Drug Info | [13] | |||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | MORF-057 | Drug Info | [4] | |||
| 2 | PN-943 | Drug Info | [10] | |||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | GS-1427 | Drug Info | [7] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7437). | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | ClinicalTrials.gov (NCT05291689) A Phase 2a, Open-label, Single-arm Study to Evaluate the Efficacy, Safety, and Tolerability of MORF-057 in Adults With Moderately to Severely Active Ulcerative Colitis (EMERALD-1). U.S.National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT04504383) A Phase 2 Randomized, Double-blind, Placebo-controlled, Parallel-group, Multi-center Study to Evaluate the Safety and Efficacy of Oral PN-943 in Subjects With Moderate to Severe Active Ulcerative Colitis. U.S.National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT01345799) A Study of TRK-170 for the Treatment of Crohn's Disease. U.S. National Institutes of Health. | |||||
| REF 7 | Clinical pipeline report, company report or official report of Gilead | |||||
| REF 8 | Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96. | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012563) | |||||
| REF 10 | Single- and Multiple-Dose Pharmacokinetics and Pharmacodynamics of PN-943, a Gastrointestinal-Restricted Oral Peptide Antagonist of alpha4beta7, in Healthy Volunteers. Clin Pharmacol Drug Dev. 2021 Nov;10(11):1263-1278. | |||||
| REF 11 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 12 | Vedolizumab: an 47 integrin inhibitor for inflammatory bowel diseases.Ann Pharmacother.2014 Dec;48(12):1629-35. | |||||
| REF 13 | Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog. Xenobiotica. 2005 Apr;35(4):373-89. | |||||
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