Top ▲

proteasome 20S subunit beta 5

Click here for help

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
Gene and Protein Information Comments
The Antimalarial targets family provides information about Plasmodium falciparum proteasome subunit beta type-5.
Previous and Unofficial Names Click here for help
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 Click here for help
Specialist databases
MEROPS T01.P01 (Hs)
Other databases
Alphafold
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]
MG-132 Peptide Ligand has a PDB structure Hs Inhibition 8.4 pKi 6
pKi 8.4 (Ki 3.7x10-9 M) [6]
Description: Inhibition of the chymotrypsin-like activity of proteasome macropain.
compound 3b [PMID: 24946214] Small molecule or natural product Bt Inhibition 8.3 pKi 7
pKi 8.3 (Ki 5.1x10-9 M) [7]
Description: Inhibition of chymotrypsin-like activity.
NIC-0102 Small molecule or natural product Hs Inhibition 8.4 pIC50 8
pIC50 8.4 (IC50 3.7x10-9 M) [8]
carfilzomib Small molecule or natural product Approved drug Hs Inhibition 8.2 pIC50 9
pIC50 8.2 (IC50 5.7x10-9 M) [9]
oprozomib Small molecule or natural product Primary target of this compound Hs Inhibition 7.5 – 8.0 pIC50 2,9
pIC50 7.5 – 8.0 (IC50 3.2x10-8 – 1x10-8 M) [2,9]
bortezomib Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Immunopharmacology Ligand Guide to Malaria Pharmacology Ligand Hs Inhibition 7.7 pIC50 5
pIC50 7.7 (IC50 2x10-8 M) [5]
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.
WLL-vs Small molecule or natural product Guide to Malaria Pharmacology Ligand Hs Inhibition 6.0 pIC50 4
pIC50 6.0 (IC50 1x10-6 M) [4]
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Antigen presentation
Immuno Process:  Cellular signalling
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Inflammation

References

Show »

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. Li H, O'Donoghue AJ, van der Linden WA, Xie SC, Yoo E, Foe IT, Tilley L, Craik CS, da Fonseca PC, Bogyo M. (2016) Structure- and function-based design of Plasmodium-selective proteasome inhibitors. Nature, 530 (7589): 233-6. [PMID:26863983]

5. 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]

6. 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]

7. 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]

8. Wu X, Sun P, Chen X, Hua L, Cai H, Liu Z, Zhang C, Liang S, Chen Y, Wu D et al.. (2022) Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity. J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.2c00523 [PMID:36063115]

9. 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 06/09/2022. Accessed on 09/12/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2406.