Resistance mutation info of target

Target General Information
Target ID T49031
Target Name Proteasome subunit beta type-5 (PSMB5) Target Info
Gene Name PSMB5
Species Homo sapiens
Uniprot ID PSB5_HUMAN
Sequence MALASVLERPLPVNQRGFFGLGGRADLLDLGPGSLSDGLSLAAPGWGVPEEPGIEMLHGT
TTLAFKFRHGVIVAADSRATAGAYIASQTVKKVIEINPYLLGTMAGGAADCSFWERLLAR
QCRIYELRNKERISVAAASKLLANMVYQYKGMGLSMGTMICGWDKRGPGLYYVDSEGNRI
SGATFSVGSGSVYAYGVMDRGYSYDLEVEQAYDLARRAIYQATYRDAYSGGAVNLYHVRE
DGWIRVSSDNVADLHEKYSGSTP [Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 537129New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21.
Ref 541528(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6391).
Ref 1572596PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo.
Mutation Info Missense: A49T
Drugs
Drug Name Bortezomib Drug Info [1559239]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 66.7 fold resistance
Drug Name PR-924 Drug Info [1559232]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 13 fold resistance
Mutation Info Missense: A49V
Drugs
Drug Name Bortezomib Drug Info [1559239]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 39.4 fold resistance
Mutation Info Missense: A50V
Drugs
Drug Name Bortezomib Drug Info [1559239]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 66.7 fold resistance
Mutation Info Missense: C52F
Drugs
Drug Name Bortezomib Drug Info [1559232]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 13 fold resistance
Mutation Info Missense: M45I
Drugs
Drug Name PR-924 Drug Info [1559232]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 13 fold resistance
Mutation Info Missense: M45V
Drugs
Drug Name PR-924 Drug Info [1559232]
Targeted Disease T lymphoblastic lymphoma/leukemia
Level of Resistance Confer 13 fold resistance
Reference
Ref 1559239Different mutants of PSMB5 confer varying bortezomib resistance in T lymphoblastic lymphoma/leukemia cells derived from the Jurkat cell line.Exp Hematol.2009 Jul;37(7):831-7.
Ref 1559232Anti-leukemic activity and mechanisms underlying resistance to the novel immunoproteasome inhibitor PR-924.Biochem Pharmacol.2014 May 1;89(1):43-51.

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