Target intelligence / Profile preview

Calcitonin gene-related peptide beta (CALCB)

Target
CALCB
Molecular classification
Peptide hormone, Neuropeptide, Endogenous ligand, Other
01

Overview

Calcitonin gene-related peptide beta (CALCB) is a 37-amino acid neuropeptide hormone and member of the calcitonin family, distinct from the more widely studied alpha-CGRP by just three amino acids in humans[3][5]. It is primarily encoded by its own gene (CALCB) and acts through the calcitonin receptor-like receptor (CALCRL) in complex with receptor activity-modifying protein 1 (RAMP1), forming a functionally unique receptor[3][5]. CALCB mediates potent vasodilatory and hypotensive effects in multiple tissues, notably participating in regulation of vascular homeostasis, blood pressure, and neurogenic inflammation. It acts as a neurotransmitter or neuromodulator, especially prominent in sensory pathways including those underlying pain and migraine. CALCB expression is dynamically regulated in response to stress, inflammation, and differentiation signals across various tissues, and dysregulation is implicated in several conditions, including cardiovascular disease, migraine, inflammatory states, and some cancers[1][3]. CGRP pathway antagonists (gepants) are clinically significant for migraine therapy but require ongoing evaluation for possible cardiovascular and healing-related risks associated with chronic CGRP blockade[3][5].

Other names
Calcitonin-related polypeptide betaCALCBCalcitonin gene-related peptide IICGRP2Beta-type CGRPCGRP-IICALC2beta-CGRPFLJ30166
02

Mechanism of action

Competitive antagonism of CGRP receptor (CLR/RAMP1 complex) to block peptide binding; Inhibition of neurogenic vasodilation and pain transmission

03

Biological functions

VasodilationRegulation of vascular toneNeurotransmitter or neuromodulator activityHormone activityModulation of pain pathwaysRegulation of inflammatory processesSignal transduction
04

Disease associations

Cardiovascular disease (e.g., hypertension, vascular tone regulation)Migraine (via modulation of pain signaling)Inflammatory disease (e.g., psoriasis)Tumor/susceptibility to certain cancers (e.g., adenoid cystic carcinoma)Lung injury (protective roles in ventilator-induced lung injury models)Other
05

Safety considerations

Potential for vascular side effects (e.g., hypertension if CGRP activity is excessively blocked)Unknown long-term effects on cardiovascular and wound healing biology
06

Interacting drugs

Gepants (class of CGRP antagonists, e.g., ubrogepant, rimegepant, atogepant, telcagepant)

1 more in the full profile.

07

Biomarkers

Circulating CGRP levels (for migraine and vascular disease research and monitoring efficacy of antagonist therapy)Genetic polymorphisms (risk assessment in certain cancers and inflammatory diseases)

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