Target Information

Target General Infomation
Target ID
T93509
Former ID
TTDC00017
Target Name
Calcitonin gene-related peptide 1
Gene Name
CALCA
Synonyms
Alpha-type CGRP; CALC1; CGRP-I; Calcitonin gene-related peptide I; CALCA
Target Type
Clinical Trial
Disease Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Function
CGRP induces vasodilation. It dilates a variety of vessels including the coronary, cerebral and systemic vasculature. Its abundance in the CNS also points toward a neurotransmitter or neuromodulator role. It also elevates platelet cAMP.
BioChemical Class
Cytotoxic amylin family
Target Validation
T93509
UniProt ID
P06881
Sequence
MGFQKFSPFLALSILVLLQAGSLHAAPFRSALESSPADPATLSEDEARLLLAALVQNYVQ
MKASELEQEQEREGSRIIAQKRACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAFG
RRRRDLQA
Drugs and Mode of Action
Drug(s) Cizolirtine Drug Info Phase 2 Neuropathic pain [536374]
Inhibitor Ac-VTHRLAGLLSRSGGVVKNNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-VTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVEHRLKGELSRKGGVV[hArg]KNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVTHQLAGLLSQSGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVTHRLAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVTH[Cit]LAGLLSRSGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVTH[Cit]LAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Ac-WVTH[hArg]LAGLLS[hArg]SGGVVRKNFVPTDVGPFAF-NH2 Drug Info [529839]
Cizolirtine Drug Info [536374]
FV-Aib-TDVGPFAF Drug Info [529839]
VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2 Drug Info [529839]
WVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2 Drug Info [529839]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome G alpha (s) signalling events
Calcitonin-like ligand receptors
WikiPathways Myometrial Relaxation and Contraction Pathways
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
References
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.

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