Drug General Information
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]
Targeted Disease	Leukemia; Myeloma
Drug Resistance Mutations	Mutation info Missense: Y373C [1], [2]
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	Leukemia; Myeloma
Drug Resistance Mutations	Mutation info Missense: C52F [3] Level of Resistance Confer 13 fold resistance
	Mutation info Missense: A49T [4] Level of Resistance Confer 66.7 fold resistance
	Mutation info Missense: A49V [4] Level of Resistance Confer 39.4 fold resistance
	Mutation info Missense: A50V [4] Level of Resistance Confer 66.7 fold resistance
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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