Target Information

Target General Information

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Target ID

T93509 (Former ID: TTDC00017)

Target Name

Calcitonin gene-related peptide 1 (CALCA)

Synonyms

Calcitonin gene-related peptide I; CGRP-I; CALCA; CALC1; Alpha-type CGRP

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Gene Name

CALCA

Target Type

Clinical trial target

[1]

Disease

[+] 1 Target-related Diseases

General pain disorder [ICD-11: 8E43]

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.

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BioChemical Class

Cytotoxic amylin family

UniProt ID

CALCA_HUMAN

Sequence

MGFQKFSPFLALSILVLLQAGSLHAAPFRSALESSPADPATLSEDEARLLLAALVQDYVQ
MKASELEQEQEREGSRIIAQKRACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAFG
RRRRDLQA

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ADReCS ID

BADD_A06440

HIT2.0 ID

T29C64

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 1 Clinical Trial Drugs

Cizolirtine

Drug Info

Phase 2

Neuropathic pain

[1]

Mode of Action

[+] 1 Modes of Action

Inhibitor

[+] 13 Inhibitor drugs

Cizolirtine

Drug Info

[1]

Ac-VTHRLAGLLSRSGGVVKNNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-VTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVEHRLKGELSRKGGVV[hArg]KNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVTHQLAGLLSQSGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVTHRLAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVTH[Cit]LAGLLSRSGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVTH[Cit]LAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

Ac-WVTH[hArg]LAGLLS[hArg]SGGVVRKNFVPTDVGPFAF-NH2

Drug Info

[2]

FV-Aib-TDVGPFAF

Drug Info

[2]

VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2

Drug Info

[2]

WVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2

Drug Info

[2]

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues. The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021). Human Similarity Proteins Human Tissue Distribution

Different Human System Profiles of Target

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Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.

The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021).

Human Similarity Proteins

Human Tissue Distribution

There is no similarity protein (E value < 0.005) for this target


Note: If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

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Reactome

[+] 2 Reactome Pathways

G alpha (s) signalling events

Calcitonin-like ligand receptors

WikiPathways

[+] 4 WikiPathways

Myometrial Relaxation and Contraction Pathways

Endothelin Pathways

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.

REF 2

Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor. J Med Chem. 2008 Dec 25;51(24):7889-97.

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