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Cellular and Molecular Life Sciences, 2006
This review describes the structure and function of prolyl endopeptidase (PEP) enzymes and how they are being evaluated as drug targets and therapeutic agents. The most well studied PEP family has a two-domain structure whose unique seven-blade beta-propeller domain works with the catalytic domain to hydrolyze the peptide bond on the carboxyl side of ...
J, Gass, C, Khosla
openaire +2 more sources
This review describes the structure and function of prolyl endopeptidase (PEP) enzymes and how they are being evaluated as drug targets and therapeutic agents. The most well studied PEP family has a two-domain structure whose unique seven-blade beta-propeller domain works with the catalytic domain to hydrolyze the peptide bond on the carboxyl side of ...
J, Gass, C, Khosla
openaire +2 more sources
Degradation of lysylbradykinin by endopeptidase 24.11 and endopeptidase 24.15
Peptides, 1995Lysylbradykinin (LBK), a potent bioactive peptide with pleiotropic actions, is the major kinin generated in the extravascular space. To explore possible mechanisms of inactivation of this peptide in tissues, we evaluated its degradation by endopeptidase 24.11 (EP 24.11) and endopeptidase 24.15 (EP 24.15), two zinc metalloenzymes widely distributed in ...
Christopher Cardozo +3 more
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2013
In the course of solubilization and purification of fusicoccin binding sites present in microsomal fractions of spinach (Spinaciaoleracea L.)leaves,some endogenous hydrolases responsible for the poor stability of the receptors were identified [1]. Among them there was a serine proteinase displaying leucine-specific proteolytic activity.To reflect its ...
ADUCCI, PATRIZIA, Ascenzi, P.
openaire +5 more sources
In the course of solubilization and purification of fusicoccin binding sites present in microsomal fractions of spinach (Spinaciaoleracea L.)leaves,some endogenous hydrolases responsible for the poor stability of the receptors were identified [1]. Among them there was a serine proteinase displaying leucine-specific proteolytic activity.To reflect its ...
ADUCCI, PATRIZIA, Ascenzi, P.
openaire +5 more sources
Prolyl endopeptidase inhibitors
Il Farmaco, 2000Selective prolyl endopeptidase inhibitors were elaborated by modification of the structure of SUAM-1221, by using a CoMFA study and protein crystallography. The most active representatives of omega-(N-hetaryl)alkanoylprolylpyrrolidines, containing 2- or 3-methylene chain links have high activity (IC50 10(-9)-10(-11)) and exhibit significant in vivo ...
Károly Kánai, István Hermecz
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Journal of the National Cancer Institute, 2014
BACKGROUND Asparaginyl endopeptidase (AEP) has been implicated in human cancer development. However, the molecular mechanisms underlying AEP regulation, including the role of pro-AEP activation, remain elusive. METHODS We investigated the regulation of
Yingying Lin +15 more
semanticscholar +1 more source
BACKGROUND Asparaginyl endopeptidase (AEP) has been implicated in human cancer development. However, the molecular mechanisms underlying AEP regulation, including the role of pro-AEP activation, remain elusive. METHODS We investigated the regulation of
Yingying Lin +15 more
semanticscholar +1 more source