Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T64213 | Target Info | |||
| Target Name | Transient receptor potential cation channel V4 (TRPV4) | ||||
| Synonyms |
Vanilloid receptor-related osmotically-activated channel; Vanilloid receptor-like protein 2; Vanilloid receptor-like channel 2; VROAC; VRL2; VRL-2; VR-OAC; TrpV4; Transient receptor potential protein 12; Transient receptor potential cation channel subfamily V member 4; TRP12; Osm-9-like TRP channel 4; OTRPC4
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| Target Type | Clinical trial Target | ||||
| Gene Name | TRPV4 | ||||
| Biochemical Class | Transient receptor potential catioin channel | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Protein kinase C epsilon (PRKCE) | Successful Target | ||||
| UniProt ID | KPCE_HUMAN | |||||
| Gene Name | PRKCE | |||||
| Synonyms |
Protein kinase C epsilon type; PKCE; PKC epsilon; NPKC-epsilon
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| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | Ki = 0.45 nM | [1] | ||
| Co-Target Name | Protein kinase C alpha (PRKCA) | Successful Target | ||||
| UniProt ID | KPCA_HUMAN | |||||
| Gene Name | PRKCA | |||||
| Synonyms |
Protein kinase C alpha type; PRKACA; PKCalpha; PKCA; PKC-alpha; PKC-A
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| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | Ki = 2.5 nM | [1] | ||
| Co-Target Name | Protein kinase C gamma (PRKCG) | Successful Target | ||||
| UniProt ID | KPCG_HUMAN | |||||
| Gene Name | PRKCG | |||||
| Synonyms |
PRKCG; PKCG; PKC-gamma
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| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | Ki = 4.9 nM | [1] | ||
| Co-Target Name | Protein kinase C delta (PRKCD) | Clinical trial Target | ||||
| UniProt ID | KPCD_HUMAN | |||||
| Gene Name | PRKCD | |||||
| Synonyms |
nPKC-delta; Tyrosine-protein kinase PRKCD; SDK1; Protein kinase C delta type catalytic subunit; Protein kinase C delta type; PKC-delta
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| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | Ki = 0.8 nM | [1] | ||
| Co-Target Name | Protein kinase C beta (PRKCB) | Clinical trial Target | ||||
| UniProt ID | KPCB_HUMAN | |||||
| Gene Name | PRKCB | |||||
| Synonyms |
Protein kinase C beta type; PRKCB1; PKCB; PKC-beta; PKC-B
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| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | Ki = 1.8 nM | [1] | ||
| Co-Target Name | Protein kinase C (PRKC) | Clinical trial Target | ||||
| UniProt ID | KPCA_HUMAN; KPCB_HUMAN; KPCD1_HUMAN; KPCD3_HUMAN; KPCD_HUMAN; KPCE_HUMAN; KPCG_HUMAN; KPCI_HUMAN; KPCL_HUMAN; KPCT_HUMAN; KPCZ_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | EC50 = 9.5 nM | [2] | ||
| Co-Target Name | RAS guanyl releasing protein 3 (RASGRP3) | Co-Target | ||||
| UniProt ID | GRP3_HUMAN | |||||
| Gene Name | RASGRP3 | |||||
| Synonyms |
Ras guanyl-releasing protein 3; Calcium and DAG-regulated guanine nucleotide exchange factor III; Guanine nucleotide exchange factor for Rap1
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| Representative Drug(s) | phorbol 12-myristate 13-acetate | Drug Info | EC50 = 82 nM | [3] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth. Bioorg Med Chem Lett. 2001 Apr 23;11(8):955-9. | ||||
| REF 2 | Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes. J Nat Prod. 2016 Oct 28;79(10):2658-66. | ||||
| REF 3 | Alpha-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands. J Med Chem. 2018 Jul 26;61(14):6261-6276. | ||||
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