Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T18477 | Target Info | |||
| Target Name | Heat shock protein 90 alpha (HSP90A) | ||||
| Synonyms |
Renal carcinoma antigen NY-REN-38; Lipopolysaccharide-associated protein 2; LPS-associated protein 2; LAP-2; Heat shock protein HSP 90-alpha; Heat shock 86 kDa; HSPCA; HSPC1; HSP90A; HSP86; HSP 86
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| Target Type | Successful Target | ||||
| Gene Name | HSP90AA1 | ||||
| Biochemical Class | Heat shock protein | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Histone deacetylase (HDAC) | Successful Target | ||||
| UniProt ID | HDAC1_HUMAN; HDAC2_HUMAN; HDAC3_HUMAN; HDAC4_HUMAN; HDAC5_HUMAN; HDAC6_HUMAN; HDAC7_HUMAN; HDAC8_HUMAN; HDAC9_HUMAN; HDA10_HUMAN; HDA11_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
Human histone deacetylase
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| Representative Drug(s) | BIIB-021 | Drug Info | IC50 ~ 1000 nM | [1] | ||
| Co-Target Name | Heat shock protein 90 beta (HSP90B) | Clinical trial Target | ||||
| UniProt ID | HS90B_HUMAN | |||||
| Gene Name | HSP90AB1 | |||||
| Synonyms |
Heat shock 84 kDa; HSP84; HSP 84
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| Representative Drug(s) | NVP-AUY922 | Drug Info | Ki = 0.064 nM | Click to Show More | [2] | |
| 2 | BIIB-021 | Drug Info | Ki = 1.7 nM | [2] | ||
| 3 | VER 50589 | Drug Info | IC50 = 28 nM | [4] | ||
| 4 | AT13387 | Drug Info | IC50 = 30 nM | [5] | ||
| 5 | Debio 0932 | Drug Info | IC50 = 38 nM | [6] | ||
| 6 | PU3 | Drug Info | IC50 = 1000 nM | [4] | ||
| Co-Target Name | Endoplasmin (HSP90B1) | Clinical trial Target | ||||
| UniProt ID | ENPL_HUMAN | |||||
| Gene Name | HSP90B1 | |||||
| Synonyms |
gp96 homolog; Tumor rejection antigen 1; TRA1; Heat shock protein 90 kDa beta member 1; GRP94; GRP-94; 94 kDa glucoseregulated protein; 94 kDa glucose-regulated protein
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| Representative Drug(s) | NVP-AUY922 | Drug Info | Ki = 4 nM | Click to Show More | [3] | |
| 2 | BIIB-021 | Drug Info | Ki = 176 nM | [3] | ||
| Co-Target Name | NF-kappa-B-activating kinase (TBK1) | Patented-recorded Target | ||||
| UniProt ID | TBK1_HUMAN | |||||
| Gene Name | TBK1 | |||||
| Synonyms |
TANK-binding kinase 1; T2K; Serine/threonine-protein kinase TBK1; NAK
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| Representative Drug(s) | Amlexanox | Drug Info | IC50 = 850 nM | [7] | ||
| Co-Target Name | Heat shock protein 75 kDa mitochondrial (TRAP1) | Co-Target | ||||
| UniProt ID | TRAP1_HUMAN | |||||
| Gene Name | TRAP1 | |||||
| Synonyms |
Heat shock protein 75 kDa, mitochondrial; HSP 75; TNFR-associated protein 1; Tumor necrosis factor type 1 receptor-associated protein; TRAP-1
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| Representative Drug(s) | NVP-AUY922 | Drug Info | Ki = 16 nM | Click to Show More | [3] | |
| 2 | BIIB-021 | Drug Info | Ki = 62 nM | [3] | ||
| 3 | NVP-AUY922 | Drug Info | IC50 = 500 nM | [8] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. Eur J Med Chem. 2018 Apr 25;150:667-677. | ||||
| REF 2 | Heat shock protein 90: inhibitors in clinical trials. J Med Chem. 2010 Jan 14;53(1):3-17. | ||||
| REF 3 | Correlation between chemotype-dependent binding conformations of HSP90alpha/beta and isoform selectivity-Implications for the structure-based design of HSP90alpha/beta selective inhibitors for treating neurodegenerative diseases. Bioorg Med Chem Lett. 2014 Jan 1;24(1):204-8. | ||||
| REF 4 | Discovery and development of heat shock protein 90 inhibitors. Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. | ||||
| REF 5 | Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening. Eur J Med Chem. 2014 May 22;79:399-412. | ||||
| REF 6 | Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. J Med Chem. 2013 Sep 12;56(17):6803-18. | ||||
| REF 7 | Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKK for the treatment of obesity. Bioorg Med Chem. 2018 Nov 1;26(20):5443-5461. | ||||
| REF 8 | New TRAP1 and Hsp90 chaperone inhibitors with cationic components: Preliminary studies on mitochondrial targeting. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2289-2293. | ||||
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