Target Information

Target General Infomation
Target ID
T97947
Former ID
TTDC00171
Target Name
Guanylyl cyclase C
Gene Name
GUCY2C
Synonyms
GC-C; GCC; HSTAR; Intestinal guanylate cyclase; STA receptor; GUCY2C
Target Type
Successful
Disease Chronic idiopathic constipation [ICD9: 564; ICD10: K59]
Crohn's disease [ICD9: 555; ICD10: K50]
Constipation; Postoperative ileus [ICD9: 537.2, 560.1, 560.31, 564.0, 777.1, 777.4; ICD10: K31.5, K56.0, K56.3, K56.7, K59.0, P76.1]
Constipation [ICD9: 564; ICD10: K59.0]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Gastrointestinal cancers [ICD9: 150-159; ICD10: C15-C26]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Function
Receptor for the E.coli heat-stable enterotoxin (E.coli enterotoxin markedly stimulates the accumulation of cGMP in mammalian cells expressing GC-C). Also activated by the endogenous peptides guanylin and uroguanylin.
BioChemical Class
Phosphorus-oxygen lyases
Target Validation
T97947
UniProt ID
P25092
EC Number
EC 4.6.1.2
Sequence
MKTLLLDLALWSLLFQPGWLSFSSQVSQNCHNGSYEISVLMMGNSAFAEPLKNLEDAVNE
GLEIVRGRLQNAGLNVTVNATFMYSDGLIHNSGDCRSSTCEGLDLLRKISNAQRMGCVLI
GPSCTYSTFQMYLDTELSYPMISAGSFGLSCDYKETLTRLMSPARKLMYFLVNFWKTNDL
PFKTYSWSTSYVYKNGTETEDCFWYLNALEASVSYFSHELGFKVVLRQDKEFQDILMDHN
RKSNVIIMCGGPEFLYKLKGDRAVAEDIVIILVDLFNDQYFEDNVTAPDYMKNVLVLTLS
PGNSLLNSSFSRNLSPTKRDFALAYLNGILLFGHMLKIFLENGENITTPKFAHAFRNLTF
EGYDGPVTLDDWGDVDSTMVLLYTSVDTKKYKVLLTYDTHVNKTYPVDMSPTFTWKNSKL
PNDITGRGPQILMIAVFTLTGAVVLLLLVALLMLRKYRKDYELRQKKWSHIPPENIFPLE
TNETNHVSLKIDDDKRRDTIQRLRQCKYDKKRVILKDLKHNDGNFTEKQKIELNKLLQID
YYNLTKFYGTVKLDTMIFGVIEYCERGSLREVLNDTISYPDGTFMDWEFKISVLYDIAKG
MSYLHSSKTEVHGRLKSTNCVVDSRMVVKITDFGCNSILPPKKDLWTAPEHLRQANISQK
GDVYSYGIIAQEIILRKETFYTLSCRDRNEKIFRVENSNGMKPFRPDLFLETAEEKELEV
YLLVKNCWEEDPEKRPDFKKIETTLAKIFGLFHDQKNESYMDTLIRRLQLYSRNLEHLVE
ERTQLYKAERDRADRLNFMLLPRLVVKSLKEKGFVEPELYEEVTIYFSDIVGFTTICKYS
TPMEVVDMLNDIYKSFDHIVDHHDVYKVETIGDAYMVASGLPKRNGNRHAIDIAKMALEI
LSFMGTFELEHLPGLPIWIRIGVHSGPCAAGVVGIKMPRYCLFGDTVNTASRMESTGLPL
RIHVSGSTIAILKRTECQFLYEVRGETYLKGRGNETTYWLTGMKDQKFNLPTPPTVENQQ
RLQAEFSDMIANSLQKRQAAGIRSQKPRRVASYKKGTLEYLQLNTTDKESTYF
Drugs and Mode of Action
Drug(s) Linaclotide Drug Info Approved Irritable bowel syndrome with constipation; Chronic idiopathic constipation [468128], [536527]
MD-1100 Drug Info Approved Constipation [532210]
Plecanatide Drug Info Approved Chronic idiopathic constipation [889446]
Guanilib Drug Info Phase 3 Crohn's disease [532471]
ISIS-GCCRrx Drug Info Phase 2 Diabetes [524485]
MD-1100 Drug Info Phase 2 Irritable bowel syndrome [536224]
MLN0264 Drug Info Phase 2 Gastrointestinal cancers [524850]
Activator Guanilib Drug Info [550622]
Linaclotide Drug Info [536527]
MD-1100 Drug Info [536224]
Modulator ISIS-GCCRrx Drug Info [543471]
MLN0264 Drug Info [549681]
Plecanatide Drug Info [556264]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
Ref 468128(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: 5017).
Ref 524485ClinicalTrials.gov (NCT01968265) Safety, Tolerability and Efficacy of ISIS-GCCRRx in Type 2 Diabetes. U.S. National Institutes of Health.
Ref 524850ClinicalTrials.gov (NCT02202759) A Study of MLN0264 in Patients With Cancer of the Stomach or Gastroesophageal Junction. U.S. National Institutes of Health.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 532471The druggable genome: Evaluation of drug targets in clinical trials suggests major shifts in molecular class and indication. Annu Rev Pharmacol Toxicol. 2014;54:9-26.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536527Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
Ref 889446Drugs@FDA (Edaravone)
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536527Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
Ref 543471(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. (Target id: 1750).
Ref 549681J Clin Oncol 31, 2013 (suppl; abstr TPS3646).
Ref 550622Guanilib, an agonist of guanylate cyclase C, is a new class of oral drug candidate that ameliorates inflammation in models of experimental colitis: O??15. Inflammatory Bowel Diseases: January 2008 - Volume 14 - Issue - p S5.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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