Resistance mutation info of drug
Drug General Information | ||||||||||||||||
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Drug ID | D0SH3I | |||||||||||||||
Drug Name | Bortezomib | |||||||||||||||
Synonyms | 179324-69-7; Velcade; Bortezomib (PS-341); UNII-69G8BD63PP; N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE; MLN-341; [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid; [(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic acid; CHEMBL325041; 69G8BD63PP; Boronic acid,; DPBA; PROSCRIPT BORONIC ACID; LPD 341; LPD-341; VELCADE (TN); Velcade (TN); Pyz-Phe-boroLeu; Bortezomib(JAN/USAN/INN); Velcade, MG-341, PS-341, Bortezomib; N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-Nalpha-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide; Bortezomib (Proteasome inhibitor); Peptide boronate | |||||||||||||||
Drug Type | Small molecular drug | |||||||||||||||
Therapeutic Class | Anticancer Agents | |||||||||||||||
Company | Takeda | |||||||||||||||
Structure | ||||||||||||||||
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] |
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Targeted Disease | Leukemia; Myeloma | |||||||||||||||
Drug Resistance Mutations |
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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] |
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Targeted Disease | Leukemia; Myeloma | |||||||||||||||
Drug Resistance Mutations |
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References | ||||||||||||||||
REF 1 | Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells. Anticancer Res. 2009 Jan;29(1):1-9. | |||||||||||||||
REF 2 | Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy. Anticancer Res. 2011 Jan;31(1):113-22. | |||||||||||||||
REF 3 | Anti-leukemic activity and mechanisms underlying resistance to the novel immunoproteasome inhibitor PR-924.Biochem Pharmacol.2014 May 1;89(1):43-51. | |||||||||||||||
REF 4 | Different 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. |
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