Target Information

Target General Infomation
Target ID
T08133
Former ID
TTDR00350
Target Name
Transient receptor potential channel 6, subfamily V
Gene Name
TRPV6
Synonyms
CaT1; Calcium channel CAT1; Calcium transport protein CaT1; ECaC2; HTRP8; Transient receptor potential cation channel subfamily V, member 6; TRPV6
Target Type
Clinical Trial
Disease Ovarian cancer [ICD9: 183; ICD10: C56]
Function
Calcium selective cation channel probably involved in Ca(2+) uptake in various tissues, including Ca(2+) reabsorption in intestine. The channel is activated by low internal calcium level, probably including intracellular calcium store depletion, and the current exhibits an inward rectification. Inactivation includes both, a rapid Ca(2+)-dependent and a slower Ca(2+)-calmodulin- dependent mechanism, the lattermay be regulated by phosphorylation. In vitro, is slowly inhibited by Mg(2+) in a voltage-independent manner. Heteromeric assembly with TRPV5 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating (By similarity).
BioChemical Class
Transient receptor potential catioin channel
UniProt ID
Q9H1D0
Sequence
MGPLQGDGGPALGGADVAPRLSPVRVWPRPQAPKEPALHPMGLSLPKEKGLILCLWSKFC
RWFQRRESWAQSRDEQNLLQQKRIWESPLLLAAKDNDVQALNKLLKYEDCKVHQRGAMGE
TALHIAALYDNLEAAMVLMEAAPELVFEPMTSELYEGQTALHIAVVNQNMNLVRALLARR
ASVSARATGTAFRRSPCNLIYFGEHPLSFAACVNSEEIVRLLIEHGADIRAQDSLGNTVL
HILILQPNKTFACQMYNLLLSYDRHGDHLQPLDLVPNHQGLTPFKLAGVEGNTVMFQHLM
QKRKHTQWTYGPLTSTLYDLTEIDSSGDEQSLLELIITTKKREARQILDQTPVKELVSLK
WKRYGRPYFCMLGAIYLLYIICFTMCCIYRPLKPRTNNRTSPRDNTLLQQKLLQEAYMTP
KDDIRLVGELVTVIGAIIILLVEVPDIFRMGVTRFFGQTILGGPFHVLIITYAFMVLVTM
VMRLISASGEVVPMSFALVLGWCNVMYFARGFQMLGPFTIMIQKMIFGDLMRFCWLMAVV
ILGFASAFYIIFQTEDPEELGHFYDYPMALFSTFELFLTIIDGPANYNVDLPFMYSITYA
AFAIIATLLMLNLLIAMMGDTHWRVAHERDELWRAQIVATTVMLERKLPRCLWPRSGICG
REYGLGDRWFLRVEDRQDLNRQRIQRYAQAFHTRGSEDLDKDSVEKLELGCPFSPHLSLP
MPSVSRSTSRSSANWERLRQGTLRRDLRGIINRGLEDGESWEYQI
Drugs and Mode of Action
Drug(s) SOR-C13 Drug Info Phase 1 Ovarian cancer [523872]
Activator 2-APB Drug Info [543864]
Inhibitor SOR-C13 Drug Info [532294]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Salivary secretion
Mineral absorption
NetPath Pathway IL2 Signaling Pathway
Pathway Interaction Database TCR signaling in na&amp
#xef
ve CD4+ T cells
Signaling events mediated by PTP1B
TCR signaling in na&amp
ve CD8+ T cells
Reactome TRP channels
WikiPathways Vitamin D Receptor Pathway
miR-targeted genes in lymphocytes - TarBase
References
Ref 523872ClinicalTrials.gov (NCT01578564) Safety and Tolerability Study of SOR-C13 in Subjects With Advanced Cancers Commonly Known to Express the TRPV6 Channel. U.S. National Institutes of Health.
Ref 532294In vivo detection of human TRPV6-rich tumors with anti-cancer peptides derived from soricidin. PLoS One. 2013;8(3):e58866.
Ref 543864(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 512).

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