Design and synthesis of multisubstrate analog inhibitors of one-carbon transfer reactions.
The design and synthesis of multisubstrate analog enzyme inhibitors offer new opportunities in the creation of potent, highly specific drug molecules. Selected examples of inhibitors of 1-carbon transfer serve to illustrate the potential of this approach. Inhibitors of indole-N-methyltransferase, L-aspartyl transcarbamoylase, and thymidylate synthase are illustrative of many compounds that have demonstrated considerable specificity and potency. Several of these inhibitors and the rationale for their syntheses are described.
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001667:Binding, Competitive; D007700:Kinetics; D013329:Structure-Activity Relationship; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D013940:Thymidylate Synthase