Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T65755 | Target Info | |||
| Target Name | Histone deacetylase (HDAC) | ||||
| Synonyms |
Human histone deacetylase
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| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | PI3-kinase alpha (PIK3CA) | Successful Target | ||||
| UniProt ID | PK3CA_HUMAN | |||||
| Gene Name | PIK3CA | |||||
| Synonyms |
p110alpha; Serine/threonine protein kinase PIK3CA; PtdIns3kinase subunit p110alpha; PtdIns3kinase subunit alpha; PtdIns-3-kinase subunit p110-alpha; PtdIns-3-kinase subunit alpha; Phosphoinositide3kinase catalytic alpha polypeptide; Phosphoinositide-3-kinase catalytic alpha polypeptide; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalytic subunit alpha; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PI3kinase subunit alpha; PI3Kalpha; PI3K-alpha; PI3-kinase subunit alpha
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| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 69 nM | [1] | ||
| Co-Target Name | PI3-kinase gamma (PIK3CG) | Successful Target | ||||
| UniProt ID | PK3CG_HUMAN | |||||
| Gene Name | PIK3CG | |||||
| Synonyms |
p120-PI3K; p110gamma; Serine/threonine protein kinase PIK3CG; PtdIns-3-kinase subunit p110-gamma; PtdIns-3-kinase subunit gamma; PtdIns-3-kinase p110; Phosphoinositol-3 kinase; Phosphoinositide-3-kinase catalytic gamma polypeptide; Phosphoinositide 3-Kinase gamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma; PI3Kgamma; PI3K-gamma; PI3K; PI3-kinase subunit gamma; PI3-kinase p110 subunit gamma
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| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 311 nM | [2] | ||
| Co-Target Name | Serine/threonine-protein kinase mTOR (mTOR) | Successful Target | ||||
| UniProt ID | MTOR_HUMAN | |||||
| Gene Name | MTOR | |||||
| Synonyms |
Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1
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| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 431 nM | [1] | ||
| Co-Target Name | Multidrug resistance protein 1 (ABCB1) | Clinical trial Target | ||||
| UniProt ID | MDR1_HUMAN | |||||
| Gene Name | ABCB1 | |||||
| Synonyms |
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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| Representative Drug(s) | CMS-024-02 | Drug Info | IC50 = 700 nM | [3] | ||
| Co-Target Name | PI3-kinase beta (PIK3CB) | Clinical trial Target | ||||
| UniProt ID | PK3CB_HUMAN | |||||
| Gene Name | PIK3CB | |||||
| Synonyms |
p110beta; PtdIns3kinase subunit p110beta; PtdIns3kinase subunit beta; PtdIns-3-kinase subunit p110-beta; PtdIns-3-kinase subunit beta; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunitbeta isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalyticsubunit beta; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta; PIK3C1; PI3kinase subunit beta; PI3Kbeta; PI3K-beta; PI3-kinase subunit beta
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| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 16 nM | [1] | ||
| Co-Target Name | Bromodomain-containing protein 4 (BRD4) | Clinical trial Target | ||||
| UniProt ID | BRD4_HUMAN | |||||
| Gene Name | BRD4 | |||||
| Synonyms |
Protein HUNK1; HUNK1
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| Representative Drug(s) | PDX-101 | Drug Info | IC50 = 27 nM | [4] | ||
| Co-Target Name | Albendazole monooxygenase (CYP3A4) | Clinical trial Target | ||||
| UniProt ID | CP3A4_HUMAN | |||||
| Gene Name | CYP3A4 | |||||
| Synonyms |
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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| Representative Drug(s) | MGCD-0103 | Drug Info | IC50 = 570 nM | Click to Show More | [5] | |
| 2 | SNDX-275 | Drug Info | IC50 = 730 nM | [5] | ||
| Co-Target Name | PI3K p110 alpha/p85 alpha (PIK3CA/PIK3R1) | Co-Target | ||||
| UniProt ID | PK3CA_HUMAN-P85A_HUMAN | |||||
| Gene Name | PIK3CA-PIK3R1 | |||||
| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 19 nM | [6] | ||
| Co-Target Name | PI3K p110 delta/p85 alpha (PIK3CD/PIK3R1) | Co-Target | ||||
| UniProt ID | PK3CD_HUMAN-P85A_HUMAN | |||||
| Gene Name | PIK3CD-PIK3R1 | |||||
| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 39 nM | [7] | ||
| Co-Target Name | PI3K p110 beta/p85 alpha (PIK3CB/PIK3R1) | Co-Target | ||||
| UniProt ID | PK3CB_HUMAN-P85A_HUMAN | |||||
| Gene Name | PIK3CB-PIK3R1 | |||||
| Representative Drug(s) | CUDC-907 | Drug Info | IC50 = 54 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J Med Chem. 2019 Aug 8;62(15):6992-7014. | ||||
| REF 2 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. J Med Chem. 2016 Jun 9;59(11):5488-504. | ||||
| REF 3 | Natural products as multidrug resistance modulators in cancer. Eur J Med Chem. 2019 Aug 15;176:268-291. | ||||
| REF 4 | Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. Bioorg Med Chem Lett. 2017 Sep 1;27(17):4051-5. | ||||
| REF 5 | The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4909-12. | ||||
| REF 6 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. J Med Chem. 2019 Apr 11;62(7):3171-3183. | ||||
| REF 7 | Designing multi-targeted agents: An emerging anticancer drug discovery paradigm. Eur J Med Chem. 2017 Aug 18;136:195-211. | ||||
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