منابع مشابه
Staurosporine, a prolyl endopeptidase inhibitor.
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...
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...
متن کاملAn Induced-Fit Mechanism for Prolyl Endopeptidase
An Induced-Fit Mechanism for Prolyl Endopeptidase Min Li 2 , Changqing Chen 3 , David R Davies 2 , and Thang K Chiu 1,2 . From the Department of Biochemistry and Molecular Biology, Louisiana State University Health Sciences Center, New Orleans, Louisiana 70112, 2 Lab of Molecular Biology, National Institute of Diabetes Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Mary...
متن کاملPoststatin, a new inhibitor of prolyl endopeptidase. VIII. Endopeptidase inhibitory activity of non-peptidyl poststatin analogues.
Non-peptidyl postatin analogues, (S)-N-substituted-2-[2-(1-acylpyrrolidinyl)]-2-oxoacetamides were synthesized and examined for their inhibitory activity against prolyl endopeptidase and cathepsin B in vitro. Many compounds showed stronger activity than natural poststatin, a pentapeptide. Among them, (S)-N-cyclohexyl-2-oxo-2-[2-(1-(3-phenoxybenzoyl)pyrrolidinyl)]ace tamide (22) and (S)-N-cycloh...
متن کاملPoststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues.
Thirty analogues of poststatin were synthesized, and their inhibitory activities against prolyl endopeptidase, human leukocyte elastase and cathepsin B were measured. The alpha-ketone was essential and the S configuration was preferable to the R configuration in the beta-substituted-beta-amino-alpha-oxopropionic acid moiety of poststatin analogues for endopeptidase inhibitory activity. The anal...
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ژورنال
عنوان ژورنال: FEBS Letters
سال: 1986
ISSN: 0014-5793
DOI: 10.1016/0014-5793(86)81118-8