trpv6

Cis-22a is a TRPV6 inhibitor (IC50 = 0.32 μM), which exhibits selectivity against related TRPV channels and calcium channels. cis-22a displays antiproliferative effects on T47D human breast cancer cells.

SOR-C13 is an inhibitor of transient receptor potential cation channel vanilloid family member 6 (TRPV6, CaT1 or CATL) with potential antineoplastic activity. TRPV6 calcium channel inhibitor SOR-C13 binds to TRPV6 and prevents the influx of calcium ions into TRPV6-expressing tumor cells. This inhibits the activation of nuclear factor of activated T-cell (NFAT) transcription complex which may result in an inhibition of calcium-dependent cancer cell proliferation and an induction of apoptosis in tumor cells overexpressing TRPV6.

SOR-C13 TFA, a truncated carboxy-terminal peptide, serves as a potent TRPV6 antagonist, demonstrating high affinity with an IC 50 value of 14 nM. TRPV6, a non-voltage-gated calcium channel linked to malignancy and poor prognosis in breast cancer, is effectively targeted by SOR-C13 TFA, indicating its anticancer activity [1].

pTH-Related Protein (1-40) (human, mouse, rat) enhances calcium absorption in rat intestinal cells by activating the PTHR1 receptor and the PKCα β signaling pathways. This compound also increases the expression of the parathyroid hormone 1 receptor (PTHR1) and four key proteins involved in transcellular calcium transport: potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium exchanger 1 (NCX1), and plasma membrane calcium ATPase 1 (PMCA1) [1].

CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) with MMAE, targeting folate receptor (FRα) and TRPV6. It exhibits high binding affinity to FRα and low affinity to TRPV6. CBP-1008 shows antitumor activity and can be utilized for research in advanced solid tumors such as colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.

CBP-1018 is a peptide-drug conjugate (PDC) composed of a dual-targeting ligand for FRα TRPV6, linked to Monomethylauristatin E. It holds promise for research in the field of breast cancer.