7 research outputs found
Spirooxazine to merooxazine interconversion in the presence and absence of zinc:Approach to a bistable photochemical switch
No full textInhibition of the Human Proteasome by Imidazoline Scaffolds
No full textThe
proteasome has emerged as the primary target for the treatment
of multiple myeloma. Unfortunately, nearly all patients develop resistance
to competitive-type proteasome inhibitors such as bortezomib. Herein,
we describe the optimization of noncompetitive proteasome inhibitors
to yield derivatives that exhibit nanomolar potency (compound <b>49</b>, IC<sub>50</sub> 130 nM) toward proteasome inhibition and
overcome bortezomib resistance. These studies illustrate the feasibility
of the development of noncompetitive proteasome inhibitors as additives
and/or alternatives to competitive proteasome inhibitors
