On November 17, 2005, Ganellin, C. Robin; Bishop, Paul B.; Bambal, Ramesh B.; Chan, Suzanne M. T.; Leblond, Bertrand; Moore, Andrew N. J.; Zhao, Lihua; Bourgeat, Pierre; Rose, Christiane; Vargas, Froylan; Schwartz, Jean-Charles published an article.Related Products of 79815-20-6 The title of the article was Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors. And the article contained the following:
The cholecystokinin-8 (CCK-8)-inactivating peptidase is a serine peptidase that has been shown to be a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10). It cleaves the neurotransmitter CCK-8 sulfate at the Met-Gly bond to give Asp-Tyr(SO3H)-Met-OH + Gly-Trp-Met-Asp-Phe-NH2. Starting from Val-Pro-NHBu, a dipeptide of submicromolar affinity that had previously been generated to serve as a lead, successive optimization at P3, P1, and then P2 gave Abu-Pro-NHBu (18, Ki = 80 nM). Further transformation (by making a benzologue) gave the indoline analog, butabindide (33) as a reversible inhibitor having nanomolar affinity (Ki = 7 nM). Retrospective anal. suggested the possibility of a general approach to designing exopeptidase inhibitors starting from the structure of the first hydrolysis product. Application of this approach to CCK-8 led to Abu-Phe-NHBu (37), but this only had Ki = 9.4 μM. Mol. modeling, to determine the min. energy conformations and explain the 1000-fold better affinity of butabindide, indicated that 37 cannot access the likely active conformation of butabindide. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Related Products of 79815-20-6
The Article related to tripeptidyl peptidase butabindide designing exopeptidase, Pharmacology: Structure-Activity and other aspects.Related Products of 79815-20-6
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles