102579-45-3Relevant academic research and scientific papers
Synthesis and evaluation of potent, highly-selective, 3-aryl-piperazinone inhibitors of protein geranylgeranyltransferase-I
Peng, Hairuo,Carrico, Dora,Thai, Van,Blaskovich, Michelle,Bucher, Cynthia,Pusateri, Erin E.,Sebti, Said M.,Hamilton, Andrew D.
, p. 1768 - 1784 (2008/02/05)
A series of compounds based on the carboxyl-terminal CAAL sequence of PGGTase-I substrates was designed and synthesized. Using piperazin-2-one as a semi-rigid scaffold, we have introduced critical pharmacophores in a well-defined arrangement to mimic the CAAL sequence. High potency and exceptional selectivity were obtained for inhibition of PGGTase-I with structures such as 45 and 70. Potency of this series of GGTIs was dependent on the presence of an l-leucine residue with a free carboxyl terminus, as well as an S configuration of the 3-aryl group. The selectivity was significantly enhanced by 5-methyl substitution on the imidazole ring and fluorine substitution on the 3-aryl group. Modification of the 6-position of the piperazinone scaffold was found to be unfavorable. Compounds 44 and 69, the corresponding methyl esters of 45 and 70, were found to selectively block processing of Rap1A by PGGTase-I in whole cells with IC50 values of 0.4 M and 0.7 M respectively. The Royal Society of Chemistry 2006.
Papain Catalysed Peptide Synthesis: Control of Amidase Activity and the Introduction of Unusual Amino Acids
Barbas, Carlos F. III,Wong, Chi-Huey
, p. 533 - 534 (2007/10/02)
Procedures for the papain catalysed synthesis of peptides containing D-amino acids and derivatives with control of the enzyme's amidase activity have been developed.
USE OF NONPROTEASES IN PEPTIDE SYNTHESIS
West, J. Blair,Wong, Chi-Huey
, p. 1629 - 1632 (2007/10/02)
Practical procedures have been developed for synthesis of peptides using lipases and esterases as catalysts.
