Table 2.

Mutations described in vitro rendering different tumor cell lines resistant to bortezomib

Cell line	Target	Mutation	Mechanism	Carfilzomib sensitivity
HT-29 adenocarcinoma	β5	Cys63Phe35	Near α-ring, inhibits bortezomib binding?	Yes35
HT-29 adenocarcinoma	Pro-peptide (β5)	Arg24Cys35	Altered recovery of proteasome activity following bortezomib exposure	Yes35
HT-29 adenocarcinoma	Pro-peptide (β5i)	Phe50Ile14	Altered recovery of proteasome activity following bortezomib exposure	Yes14
Jurkat cells	β5	Ala108Thr36	Reduces affinity between bortezomib and the chymotrypsin-like active site	Unknown
Jurkat cells	β5	Ala49Val37	Reduces affinity between bortezomib and the chymotrypsin-like active site	Unknown
Jurkat cells	β5	Ala49Thr and Ala50Val37	Reduces affinity between bortezomib and the chymotrypsin-like active site	Unknown
THP-1 KMS-11/OPM-2	β5	Ala49Thr12,38	Reduces affinity between bortezomib and the chymotrypsin-like active site	Unknown