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Diabetes Therapy
Stereospecific recognition of AS-3201 reveals pathway for improved potency and stability
March 6th, 2006
Stereospecific recognition of AS-3201 reveals role of specific binding by serum albumin involved in improved potency and stability. "AS-3201 [(3R)-2'-(4-bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4'(1'H)-pyrrolo[1,2-a]jpyrazine]-1'2,3',5(2'H)-tetrone] is a structurally novel and stereospecifically potent aldose reductase (AKR1B; EC 1.1.1.21) inhibitor, which contains a succinimide ring that undergoes ring-opening at physiological pH levels. To delineate intermolecular interactions governing its favorable pharmacokinetic profile, the interaction of AS-3201 (R-isomer) with plasma proteins, especially human serum albumin (HSA), was examined in comparison with that of the...
Source: Obesity & Diabetes Week (2006-03-06)
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