Resistance mutation info of drug

Drug General Information
Drug ID D0SH3I
Drug Name Bortezomib Drug Info
Drug Type Small molecular drug
Therapeutic Class Anticancer Agents
Company Takeda
Structure D0SH3I
Drug Resistance Mutations
Target Name Fibroblast growth factor receptor 3 (FGFR3) Target Info
Gene Name FGFR3
Uniprot ID FGFR3_HUMAN
Species Homo sapiens
Reference Sequence MGAPACALALCVAVAIVAGASSESLGTEQRVVGRAAEVPGPEPGQQEQLVFGSGDAVELS
CPPPGGGPMGPTVWVKDGTGLVPSERVLVGPQRLQVLNASHEDSGAYSCRQRLTQRVLCH
FSVRVTDAPSSGDDEDGEDEAEDTGVDTGAPYWTRPERMDKKLLAVPAANTVRFRCPAAG
NPTPSISWLKNGREFRGEHRIGGIKLRHQQWSLVMESVVPSDRGNYTCVVENKFGSIRQT
YTLDVLERSPHRPILQAGLPANQTAVLGSDVEFHCKVYSDAQPHIQWLKHVEVNGSKVGP
DGTPYVTVLKTAGANTTDKELEVLSLHNVTFEDAGEYTCLAGNSIGFSHHSAWLVVLPAE
EELVEADEAGSVYAGILSYGVGFFLFILVVAAVTLCRLRSPPKKGLGSPTVHKISRFPLK
RQVSLESNASMSSNTPLVRIARLSSGEGPTLANVSELELPADPKWELSRARLTLGKPLGE
GCFGQVVMAEAIGIDKDRAAKPVTVAVKMLKDDATDKDLSDLVSEMEMMKMIGKHKNIIN
LLGACTQGGPLYVLVEYAAKGNLREFLRARRPPGLDYSFDTCKPPEEQLTFKDLVSCAYQ
VARGMEYLASQKCIHRDLAARNVLVTEDNVMKIADFGLARDVHNLDYYKKTTNGRLPVKW
MAPEALFDRVYTHQSDVWSFGVLLWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCT
HDLYMIMRECWHAAPSQRPTFKQLVEDLDRVLTVTSTDEYLDLSAPFEQYSPGGQDTPSS
SSSGDDSVFAHDLLPPAPPSSGGSRT [Homo sapiens]
Targeted Disease Myeloma
Drug Resistance Mutations
Mutation info Missense: Y373C [555702], [555792]
Target Name Proteasome subunit beta type-5 (PSMB5) Target Info
Gene Name PSMB5
Uniprot ID PSB5_HUMAN
Species Homo sapiens
Reference Sequence MALASVLERPLPVNQRGFFGLGGRADLLDLGPGSLSDGLSLAAPGWGVPEEPGIEMLHGT
TTLAFKFRHGVIVAADSRATAGAYIASQTVKKVIEINPYLLGTMAGGAADCSFWERLLAR
QCRIYELRNKERISVAAASKLLANMVYQYKGMGLSMGTMICGWDKRGPGLYYVDSEGNRI
SGATFSVGSGSVYAYGVMDRGYSYDLEVEQAYDLARRAIYQATYRDAYSGGAVNLYHVRE
DGWIRVSSDNVADLHEKYSGSTP [Homo sapiens]
Targeted Disease T lymphoblastic lymphoma/leukemia
Drug Resistance Mutations
Mutation info Missense: A49T [1559239]
Level of Resistance Confer 66.7 fold resistance
Mutation info Missense: A49V [1559239]
Level of Resistance Confer 39.4 fold resistance
Mutation info Missense: A50V [1559239]
Level of Resistance Confer 66.7 fold resistance
Mutation info Missense: C52F [1559232]
Level of Resistance Confer 13 fold resistance
References
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 555702Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells. Anticancer Res. 2009 Jan;29(1):1-9.
Ref 555792Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy. Anticancer Res. 2011 Jan;31(1):113-22.
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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