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proteasome 20S subunit beta 5

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Target not currently curated in GtoImmuPdb

Target id: 2406

Nomenclature: proteasome 20S subunit beta 5

Family: T1: Proteasome

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 263 14q11.2 PSMB5 proteasome 20S subunit beta 5
Mouse - 264 14 27.86 cM Psmb5 proteasome (prosome, macropain) subunit, beta type 5
Rat - 263 15p13 Psmb5 proteasome 20S subunit beta 5
Previous and Unofficial Names Click here for help
MB1 | macropain epsilon chain | multicatalytic endopeptidase complex epsilon chain | proteasome beta 5 subunit | proteasome chain 6 | proteasome epsilon chain | proteasome subunit X | proteasome (prosome, macropain) subunit, beta type, 5 | proteasome (prosome, macropain) subunit, beta type 5 | proteasome (prosome | proteasome subunit beta 5
Database Links Click here for help
Specialist databases
MEROPS T01.P01 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.25.1

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
ixazomib Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.0 pKi 3
pKi 9.0 (Ki 9.3x10-10 M) [3]
compound 5b [PMID: 16686537] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.4 pKi 5
pKi 8.4 (Ki 3.7x10-9 M) [5]
Description: Inhibition of the chymotrypsin-like activity of proteasome macropain.
compound 3b [PMID: 24946214] Small molecule or natural product Bt Inhibition 8.3 pKi 6
pKi 8.3 (Ki 5.1x10-9 M) [6]
Description: Inhibition of chymotrypsin-like activity.
carfilzomib Small molecule or natural product Approved drug Hs Inhibition 8.2 pIC50 7
pIC50 8.2 (IC50 5.7x10-9 M) [7]
oprozomib Small molecule or natural product Primary target of this compound Hs Inhibition 7.5 – 8.0 pIC50 2,7
pIC50 7.5 – 8.0 (IC50 3.2x10-8 – 1x10-8 M) [2,7]
bortezomib Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 2x10-8 M) [4]
KZR-616 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.2 pIC50 1
pIC50 6.2 (IC50 6.88x10-7 M) [1]
Description: Inhibition of proteolytic activity measured in MOLT-4 (human T cell leukemia) cell lysate using the ProCISE ELISA.
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0002479 antigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependent TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 4 GO processes
GO:0000209 protein polyubiquitination TAS
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0050852 T cell receptor signaling pathway TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes
GO:0033209 tumor necrosis factor-mediated signaling pathway TAS
GO:0070498 interleukin-1-mediated signaling pathway TAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0050852 T cell receptor signaling pathway TAS
Immuno Process:  Immune system development
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0002223 stimulatory C-type lectin receptor signaling pathway TAS

References

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1. Johnson HWB, Lowe E, Anderl JL, Fan A, Muchamuel T, Bowers S, Moebius DC, Kirk C, McMinn DL. (2018) Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem, 61 (24): 11127-11143. [PMID:30380863]

2. Kale AJ, Moore BS. (2012) Molecular mechanisms of acquired proteasome inhibitor resistance. J Med Chem, 55 (23): 10317-27. [PMID:22978849]

3. Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F et al.. (2010) Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res, 70 (5): 1970-80. [PMID:20160034]

4. Nakamura H, Watanabe M, Ban HS, Nabeyama W, Asai A. (2009) Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors. Bioorg Med Chem Lett, 19 (12): 3220-4. [PMID:19428245]

5. Rydzewski RM, Burrill L, Mendonca R, Palmer JT, Rice M, Tahilramani R, Bass KE, Leung L, Gjerstad E, Janc JW et al.. (2006) Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors. J Med Chem, 49 (10): 2953-68. [PMID:16686537]

6. Troiano V, Scarbaci K, Ettari R, Micale N, Cerchia C, Pinto A, Schirmeister T, Novellino E, Grasso S, Lavecchia A et al.. (2014) Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors. Eur J Med Chem, 83: 1-14. [PMID:24946214]

7. Zhou HJ, Aujay MA, Bennett MK, Dajee M, Demo SD, Fang Y, Ho MN, Jiang J, Kirk CJ, Laidig GJ et al.. (2009) Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J Med Chem, 52 (9): 3028-38. [PMID:19348473]

How to cite this page

T1: Proteasome: proteasome 20S subunit beta 5. Last modified on 12/09/2019. Accessed on 12/05/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2406.