proteasome 20S subunit beta 5 | T1: Proteasome | IUPHAR/BPS Guide to PHARMACOLOGY

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proteasome 20S subunit beta 5

Target not currently curated in GtoImmuPdb

Target id: 2406

Nomenclature: proteasome 20S subunit beta 5

Family: T1: Proteasome

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 263 14q11.2 PSMB5 proteasome 20S subunit beta 5
Mouse - 264 14 C2-D1 Psmb5 proteasome (prosome, macropain) subunit, beta type 5
Rat - 263 15p13 Psmb5 proteasome 20S subunit beta 5
Previous and Unofficial Names
macropain epsilon chain | MB1 | 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
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
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.25.1

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 Value Parameter Reference
ixazomib Hs Inhibition 9.0 pKi 3
pKi 9.0 (Ki 9.3x10-10 M) [3]
compound 5b [PMID: 16686537] 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] Bt Inhibition 8.3 pKi 6
pKi 8.3 (Ki 5.1x10-9 M) [6]
Description: Inhibition of chymotrypsin-like activity.
carfilzomib Hs Inhibition 8.2 pIC50 7
pIC50 8.2 (IC50 5.7x10-9 M) [7]
oprozomib Hs Inhibition 7.5 – 8.0 pIC50 2,7
pIC50 7.5 – 8.0 (IC50 3.2x10-8 – 1x10-8 M) [2,7]
bortezomib Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 2x10-8 M) [4]
KZR-616 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

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 19/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2406.