2-APB, Ca2+ release modulator

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

TRPV1 also known as the capsaicin or vanilloid receptor 1 is a protein that acts as an ion channel primarily allowing the passage of calcium ions. It has an approximate molecular mass of 95 kDa and is expressed in sensory neurons particularly in the dorsal root ganglia. TRPV1 is sensitive to heat acidic conditions and natural compounds like capsaicin and plays a role in the perception of pain and heat. The Vitamin D Receptor (VDR) is a nuclear receptor that binds vitamin D and its active form with a molecular mass of approximately 48 kDa and is expressed in various tissues including the intestine bone and kidney regulating calcium and phosphorus balance. TRPV2 similar to TRPV1 is also an ion channel protein involved in detecting noxious heat with a molecular mass of about 86 kDa. It is mainly expressed in the central and peripheral nervous systems. Cytochrome P450 3A4 (CYP3A4) is involved in the metabolism of various xenobiotics and drugs having a molecular weight of roughly 57 kDa and is prominently expressed in the liver.

Biological function summary

TRPV1 and TRPV2 are integral in pain modulation and detection of temperature changes contributing to the body's response to external stimuli and potentially influencing behavioral responses. TRPM2 another member of the transient receptor potential channel family functions as a cation channel activated by oxidative stress affecting Ca2+ release. The Vitamin D Receptor modulates gene transcription in numerous cells facilitating calcium absorption and immune system function. It works in tandem with proteins such as cytochrome P450 enzymes including CYP3A4 to regulate vitamin D3 metabolism. 15-Lipoxygenase-1 (15-LOX-1) metabolizes polyunsaturated fatty acids particularly arachidonic acid in inflammatory processes. All these proteins contribute significantly to maintaining cellular homeostasis and communication.

Pathways

TRPV1 is associated with the nociceptive pain pathway where it interacts with other proteins like TRPV2 to mediate thermal and inflammatory pain. VDR plays an important role in the vitamin D signaling pathway aiding in calcium homeostasis and bone health with interactions involving proteins like CYP3A4 in metabolic pathways. TDP1 a phosphodiesterase involved in DNA repair interacts with proteins within the DNA damage response pathway ultimately affecting cellular survival and response to genotoxic stress. Similarly 15-LOX-2 functions in pathways linked to lipid metabolism.

Associated diseases and disorders

TRPV1 shows relevance to conditions such as chronic pain and inflammatory diseases where it is often overactive. It maintains connections with related receptors like TRPV3. The Vitamin D Receptor links to osteoporosis through its role in calcium regulation and bone density. Variants in the VDR gene may alter susceptibility to certain cancers due to disordered control of cellular proliferation. Cytochrome P450 enzymes including CYP3A4 relate to drug metabolism disorders and conditions resulting from exposure to toxic substances. Alterations in 15-Lipoxygenase-1 are associated with asthma involving the regulation of inflammatory mediators. These associations highlight the multifaceted roles of these targets in human health and disease.