heat shock protein 90 beta family member 1

Target id: 2904

Nomenclature: heat shock protein 90 beta family member 1

Abbreviated Name: HSP90B1

Family: Heat shock proteins

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     heat shock protein 90 beta family member 1 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 803 12q24.2-q24.3 HSP90B1 heat shock protein 90 beta family member 1
Mouse - 802 Chromosome 10, 43.05 cM Hsp90b1 heat shock protein 90, beta (Grp94), member 1
Rat - 804 7q13 Hsp90b1 heat shock protein 90 beta family member 1
Previous and Unofficial Names
Endoplasmin | GRP-94 | HSP90B1
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
18c [PMID: 25901531] Hs Inhibition 6.7 pIC50 1
pIC50 6.7 (IC50 2.2x10-7 M) [1]
semapimod Hs Inhibition 6.4 – 6.7 pIC50 6
pIC50 6.4 – 6.7 (IC50 4x10-7 – 2x10-7 M) [6]
Immunopharmacology Comments
HSP90B1 is an endoplasmic reticulum chaperone required for proper folding and cell surface export of newly synthesized Toll-like receptor and integrin (CD11a, CD18 and CD49d) proteins. In its absence TLR responses are ablated, and there is no innate response to microbial stimuli [3].[8]. HSP90B1 binding ligands which inhibit its association with other proteins are being investigated as anti-inflammatory agents (e.g. semapimod). HSP90B1-based autologous protein complexes isolated from cancer cells (e.g. vitespen [7], in Phase 3 clinical trial [4]) are under scrutiny as potential anti-cancer vaccine immunotherapeutics [2,5].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process ID:  2
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  toll-like receptor signaling pathway (GO:0002224) TAS
References: 
Immuno Process:  Antigen presentation
Immuno Process ID:  3
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  receptor-mediated endocytosis (GO:0006898) TAS
References: 
Immuno Process:  Immune regulation
Immuno Process ID:  6
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  toll-like receptor signaling pathway (GO:0002224) TAS
References: 
Immuno Process:  Cellular signalling
Immuno Process ID:  11
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  toll-like receptor signaling pathway (GO:0002224) TAS
ubiquitin-dependent ERAD pathway (GO:0030433) IMP
References: 

References

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1. Patel HJ, Patel PD, Ochiana SO, Yan P, Sun W, Patel MR, Shah SK, Tramentozzi E, Brooks J, Bolaender A et al.. (2015) Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94. J. Med. Chem.58 (9): 3922-43. [PMID:25901531]

2. Randazzo M, Terness P, Opelz G, Kleist C. (2012) Active-specific immunotherapy of human cancers with the heat shock protein Gp96-revisited. Int. J. Cancer130 (10): 2219-31. [PMID:22052568]

3. Randow F, Seed B. (2001) Endoplasmic reticulum chaperone gp96 is required for innate immunity but not cell viability. Nat. Cell Biol.3 (10): 891-6. [PMID:11584270]

4. Testori A, Richards J, Whitman E, Mann GB, Lutzky J, Camacho L, Parmiani G, Tosti G, Kirkwood JM, Hoos A et al.. (2008) Phase III comparison of vitespen, an autologous tumor-derived heat shock protein gp96 peptide complex vaccine, with physician's choice of treatment for stage IV melanoma: the C-100-21 Study Group. J. Clin. Oncol.26 (6): 955-62. [PMID:18281670]

5. Tosti G, Cocorocchio E, Pennacchioli E, Ferrucci PF, Testori A, Martinoli C. (2014) Heat-shock proteins-based immunotherapy for advanced melanoma in the era of target therapies and immunomodulating agents. Expert Opin Biol Ther14 (7): 955-67. [PMID:24670226]

6. Wang J, Grishin AV, Ford HR. (2016) Experimental Anti-Inflammatory Drug Semapimod Inhibits TLR Signaling by Targeting the TLR Chaperone gp96. J. Immunol.196 (12): 5130-7. [PMID:27194788]

7. Wood CG, Mulders P. (2009) Vitespen: a preclinical and clinical review. Future Oncol5 (6): 763-74. [PMID:19663726]

8. Yang Y, Liu B, Dai J, Srivastava PK, Zammit DJ, Lefran├žois L, Li Z. (2007) Heat shock protein gp96 is a master chaperone for toll-like receptors and is important in the innate function of macrophages. Immunity26 (2): 215-26. [PMID:17275357]

How to cite this page

Heat shock proteins: heat shock protein 90 beta family member 1. Last modified on 08/05/2017. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2904.