Prolyl Endopeptidase Inhibitors from the Underground Part of Rhodiola sachalinensis
نویسندگان
چکیده
منابع مشابه
Structure activity relationship of inhibitors specific for prolyl endopeptidase.
Structural requirements of N-blocked L-proline derivatives as specific inhibitors for prolyl endopeptidase were investigated using a series of substrate analogs. Replacement of L-proline by its D-isomer remarkably reduced the inhibition. Introduction of a sulfur atom in proline and/or in the penultimate pyrrolidine rings significantly increased the inhibition, but the introduction of oxygen rat...
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Prolyl endopeptidase (PEP, EC 3.4.21.26) has been proposed to play a role in degradation of proline-containing neuropeptides involved in the processes of learning and memory, e.g., vasopressin, substance P, and thyrotropin-releasing hormone (TRH). In the course of our search for bioactive constituents in medicinal plants, we studied the PEP inhibitory constituents of the roots of Lindera strych...
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anti-umnesic efTect on Alzheimer's rats.fi) In PCI2・ h cells staurosporine blocked NGF-induced neuriLe outgrowth at low doses. but at hLgher doses PCI2h cclls responded te staurospovine blr' rupid generation of neurites.4) The meehanisms of neurite outgrewth prompted by staurosporine might be difTl:Fent from that ofNGF. dB-cAMP, or infection witli a retrovirus carr},ing the v-src oncogene.4] It...
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Korea Research Institute of Bioscience and Biotechnology, KIST, P. O. Box 115, Yusong, Taejon 305-600, Korea f Dept. of Agricultural Chemistry, College of Agriculture, Kyungpook National University, 1370, Sankyuk-Dong, Taegu 702-701, Korea ft Department of Microbiology, College of Natural Sciences, Pusan National University, Pusan 609-735, Korea m The Institute of Physical and Chemical Research...
متن کاملInduced-fit Mechanism for Prolyl Endopeptidase*
Prolyl peptidases cleave proteins at proline residues and are of importance for cancer, neurological function, and type II diabetes. Prolyl endopeptidase (PEP) cleaves neuropeptides and is a drug target for neuropsychiatric diseases such as post-traumatic stress disorder, depression, and schizophrenia. Previous structural analyses showing little differences between native and substrate-bound st...
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ژورنال
عنوان ژورنال: CHEMICAL & PHARMACEUTICAL BULLETIN
سال: 2001
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.49.396