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heat shock protein 90 alpha family class A member 1

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Target id: 2905

Nomenclature: heat shock protein 90 alpha family class A member 1

Abbreviated Name: HSP90AA1

Family: Heat shock proteins

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 732 14q32.31 HSP90AA1 heat shock protein 90 alpha family class A member 1
Mouse - 733 12 60.75 cM Hsp90aa1 heat shock protein 90, alpha (cytosolic), class A member 1
Rat - 14 6q32 Hsp90aa1 heat shock protein 90 alpha family class A member 1
Previous and Unofficial Names Click here for help
HSP90AA1
Database Links Click here for help
Alphafold P07900 (Hs), P07901 (Mm), P82996 (Rn)
CATH/Gene3D 3.30.565.10
ChEMBL Target CHEMBL3880 (Hs), CHEMBL4197 (Mm)
Ensembl Gene ENSG00000080824 (Hs), ENSMUSG00000021270 (Mm), ENSRNOG00000059714 (Rn)
Entrez Gene 3320 (Hs), 15519 (Mm), 299331 (Rn)
Human Protein Atlas ENSG00000080824 (Hs)
KEGG Gene hsa:3320 (Hs), mmu:15519 (Mm), rno:299331 (Rn)
Pharos P07900 (Hs)
RefSeq Nucleotide NM_005348 (Hs), NM_010480 (Mm), NM_175761 (Rn)
RefSeq Protein NP_005339 (Hs), NP_034610 (Mm), NP_786937 (Rn)
SynPHARM 84900 (in complex with alvespimycin)
83738 (in complex with BIIB021)
83739 (in complex with SNX0723)
UniProtKB P07900 (Hs), P07901 (Mm), P82996 (Rn)
Wikipedia HSP90AA1 (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ganetespib Small molecule or natural product Ligand has a PDB structure Hs Inhibition >9.0 pKd 4
⤷ pKd >9.0 (Kd <1x10-9 M) [4]
retaspimycin hydrochloride Small molecule or natural product Hs Inhibition 6.9 pEC50 2
⤷ pEC50 6.9 (EC50 1.19x10-7 M) [2]
BIIB021 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 1
⤷ pIC50 8.7 (IC50 2x10-9 M) [1]
SNX0723 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 1
⤷ pIC50 8.5 (IC50 3x10-9 M) [1]
alvespimycin Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.4 pIC50 3
⤷ pIC50 8.4 (IC50 4.5x10-9 M) [3]
ganetespib Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.3 pIC50 5
⤷ pIC50 8.3 (IC50 5x10-9 M) [5]
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Immune system development
Immuno Process:  T cell (activation)

References

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1. Ernst JT, Liu M, Zuccola H, Neubert T, Beaumont K, Turnbull A, Kallel A, Vought B, Stamos D. (2014) Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases. Bioorg Med Chem Lett, 24 (1): 204-8. [PMID:24332488]

2. Ge J, Normant E, Porter JR, Ali JA, Dembski MS, Gao Y, Georges AT, Grenier L, Pak RH, Patterson J et al.. (2006) Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. J Med Chem, 49 (15): 4606-15. [PMID:16854066]

3. Kung PP, Funk L, Meng J, Collins M, Zhou JZ, Johnson MC, Ekker A, Wang J, Mehta P, Yin MJ et al.. (2008) Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. Bioorg Med Chem Lett, 18 (23): 6273-8. [PMID:18929486]

4. Schuetz DA, de Witte WEA, Wong YC, Knasmueller B, Richter L, Kokh DB, Sadiq K, Bosma R, Nederpelt I, Heitman LH et al.. K4DD drug target binding kinetics data. ,. DOI: 10.6019/CHEMBL3885741

5. Taldone T, Patel PD, Patel M, Patel HJ, Evans CE, Rodina A, Ochiana S, Shah SK, Uddin M, Gewirth D et al.. (2013) Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. J Med Chem, 56 (17): 6803-18. [PMID:23965125]

How to cite this page

Heat shock proteins: heat shock protein 90 alpha family class A member 1. Last modified on 03/04/2024. Accessed on 01/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2905.