Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T32262
|
||||
Former ID |
TTDC00093
|
||||
Target Name |
Calcitoningene-related peptide type 1 receptor
|
||||
Gene Name |
CALCRL
|
||||
Synonyms |
CGRP receptor 1; CGRP type 1 receptor; Calcitoningene-related peptide 1 receptor; Calcitoninreceptor-like receptor; CALCRL
|
||||
Target Type |
Clinical Trial
|
||||
Disease | Migraine [ICD9: 346; ICD10: G43] | ||||
Migraine; Cluster headaches [ICD9: 339.00, 339.01, 339.02, 346; ICD10: G43, G44.0] | |||||
Function |
Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2. The activity of thisreceptor is mediated by G proteins which activate adenylyl cyclase.
|
||||
BioChemical Class |
GPCR secretin
|
||||
Target Validation |
T32262
|
||||
UniProt ID | |||||
Sequence |
MEKKCTLNFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN |
||||
Structure |
3AQF; 3N7P; 3N7R; 3N7S
|
||||
Drugs and Mode of Action | |||||
Drug(s) | AMG 334 | Drug Info | Phase 2 | Migraine | [524809] |
BI-44370 TA | Drug Info | Phase 2 | Migraine | [522435] | |
BMS-927711 | Drug Info | Phase 2 | Migraine | [523614] | |
MK-3207 | Drug Info | Phase 2 | Migraine | [522371] | |
Olcegepant | Drug Info | Phase 2 | Migraine | [524842], [542045] | |
Telcagepant | Drug Info | Phase 2 | Migraine; Cluster headaches | [531970], [542049] | |
LBR-101 | Drug Info | Phase 1 | Migraine | [532603] | |
Modulator | AMG 334 | Drug Info | [544443] | ||
Olcegepant | Drug Info | ||||
Antagonist | BI-44370 TA | Drug Info | [531309] | ||
BMS-927711 | Drug Info | [532462] | |||
MK-3207 | Drug Info | [530631] | |||
Telcagepant | Drug Info | [537202], [537267], [537377] | |||
Inhibitor | BMS-694153 | Drug Info | [529618] | ||
EPIMER A | Drug Info | [530247] | |||
FV-Aib-TDVGPFAF | Drug Info | [527974] | |||
FV-Hyp-TDVGPFAF | Drug Info | [527974] | |||
FV-Tic-TDVGPFAF | Drug Info | [527974] | |||
FVATDVGPFAF | Drug Info | [527974] | |||
FVPTDVG-Tic-FAF-Tic | Drug Info | [527974] | |||
FVPTDVGAFAF | Drug Info | [527974] | |||
FVPTDVGPFAF | Drug Info | [527974] | |||
HCGRPalpha | Drug Info | [529789] | |||
ISOMER A | Drug Info | [530247] | |||
Pathways | |||||
References | |||||
Ref 522371 | ClinicalTrials.gov (NCT00712725) MK3207 for Treatment of Acute Migraines (3207-005). U.S. National Institutes of Health. | ||||
Ref 522435 | ClinicalTrials.gov (NCT00751803) BI 44370 TA in Acute Migraine Attack. U.S. National Institutes of Health. | ||||
Ref 523614 | ClinicalTrials.gov (NCT01430442) Dose Ranging Study of a Drug for the Treatment of Acute Migraine. U.S. National Institutes of Health. | ||||
Ref 524809 | ClinicalTrials.gov (NCT02174861) A Study to Assess the Long-term Safety and Efficacy of AMG 334 in Chronic Migraine Prevention.. U.S. National Institutes of Health. | ||||
Ref 524842 | ClinicalTrials.gov (NCT02198339) Efficacy, Safety, Tolerability and Pharmacokinetics of BIBN 4096 BS Versus Placebo in the Treatment of a Single Attack of Acute Migraine Headache. U.S. National Institutes of Health. | ||||
Ref 531970 | ACS chemical neuroscience molecule spotlight on Telcagepant (MK-0974). ACS Chem Neurosci. 2011 Jul 20;2(7):334-5. | ||||
Ref 532603 | Safety and tolerability of LBR-101, a humanized monoclonal antibody that blocks the binding of CGRP to its receptor: Results of the Phase 1 program. Cephalalgia. 2013 Dec 23;34(7):483-492. | ||||
Ref 527974 | J Med Chem. 2006 Jan 26;49(2):616-24.Identification of the key residue of calcitonin gene related peptide (CGRP) 27-37 to obtain antagonists with picomolar affinity at the CGRP receptor. | ||||
Ref 529618 | J Med Chem. 2008 Aug 28;51(16):4858-61. Epub 2008 Jul 30.Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure. | ||||
Ref 529789 | J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. | ||||
Ref 530247 | Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. Epub 2009 Jun 17.The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists. | ||||
Ref 530631 | J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. Epub 2010 Jan 11.Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. | ||||
Ref 531309 | BI 44370 TA, an oral CGRP antagonist for the treatment of acute migraine attacks: results from a phase II study. Cephalalgia. 2011 Apr;31(5):573-84. | ||||
Ref 532462 | BMS-927711 for the acute treatment of migraine: a double-blind, randomized, placebo controlled, dose-ranging trial. Cephalalgia. 2014 Feb;34(2):114-25. | ||||
Ref 532603 | Safety and tolerability of LBR-101, a humanized monoclonal antibody that blocks the binding of CGRP to its receptor: Results of the Phase 1 program. Cephalalgia. 2013 Dec 23;34(7):483-492. | ||||
Ref 537202 | A flexible and high throughput liquid chromatography-tandem mass spectrometric assay for the quantitation of telcagepant in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 May 15;877(14-15):1465-71. Epub 2009 Mar 18. | ||||
Ref 537267 | Elimination of diastereomer interference to determine Telcagepant (MK-0974) in human plasma using on-line turbulent-flow technology and off-line solid-phase extraction coupled with liquid chromatography/tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Jun 1;877(16-17):1634-42. Epub 2009 Apr 8. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.