Home
Resources
Publications
Design of (omega-N-(O-acyl)hydroxy Amid) Aminodicarboxylic Acid Pyrrolidides as Potent Inhibitors of Proline-Specific Peptidases

Design of (omega-N-(O-acyl)hydroxy Amid) Aminodicarboxylic Acid Pyrrolidides as Potent Inhibitors of Proline-Specific Peptidases

H U Demuth, D Schlenzig, A Schierhorn, G Grosche, M P Chapot-Chartier, J C Gripon

FEBS Lett. 1993 Mar 29;320(1):23-7.

PMID: 8096464

Abstract:

A novel class of competitive, acylating inhibitors for the proline-specific peptidases: dipeptidyl peptidase IV, dipeptidyl peptidase II and prolyl endopeptidase, has been developed. The inhibitor molecules combine the efficacy of aminoacyl pyrrolidides and the potential transacylating capability of diacyl hydroxyl amines. The N-terminal deblocked inhibitors are potent reversible inhibitors of porcine kidney dipeptidyl peptidase IV, human placenta dipeptidyl peptidase II exhibiting Ki values in the microM range. Boc-protected (omega-N-hydroxy acyl amid) aminodiacarboxylic acid pyrrolidides inhibit substrate hydrolysis by prolyl endopeptidases from different sources competitively reaching Ki values of 30 nM to 60 microM. Additionally, alpha-N-BOC-(omega-N-hydroxy acetyl) glutaminyl pyrrolidide modifies human placenta prolyl endopeptidase in a time-dependent reaction.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR42415189	Dipeptidyl Peptidase IV human			Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: