Molecular modelling and site-directed mutagenesis of the active site of endothelin-converting enzyme
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چکیده
منابع مشابه
Molecular modelling and site-directed mutagenesis of the active site of endothelin-converting enzyme.
Mammalian endothelin-converting enzyme is a membrane-bound metalloprotease; its C-terminal domain contains sequence motifs characteristic of zinc metalloproteases. We examined residues expected from molecular modelling to be important for substrate binding using selectively mutated recombinant rat ECE-1alpha expressed in CHO cells. A conserved N-A-Ar-Ar (Ar = aromatic) motif is likely to be imp...
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Endothelin-converting enzyme-2 (ECE-2), a member of M13 family of zinc metallopeptidases, has previously been shown to process a number of neuropeptides including those derived from prodynorphin, proenkephalin, proSAAS, and amyloid precursor protein. ECE-2, unlike ECE-1, exhibits restricted neuroendocrine distribution and acidic pH optimum; it is consistent with a role in the regulation of neur...
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Derivatives of phenyl-keto butenoic acids have been reported to be inhibitors of pyruvate decarboxylase, (PDC). The inhibition of transketolase, a thiamine requiring enzyme such as PDF, by meta nitrophenyl derivative of 2-oxo-3-butenoic acid (MNPB) is reported here. These studies indicate that the inhibitor binds to the enzyme at the active site. A two-step inhibition was observed, first th...
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Earlier covalent modification experiments indicated that histidine, arginine, and carboxylic acid residues were involved in the catalytic mechanism of the acid phosphatase enzyme from human prostate. The present study utilizes site-directed mutagenesis to evaluate the catalytic importance of 7 residues of human prostatic phosphatase, namely His12, His257, Asp258, Arg11, Arg15, Arg54, and Arg79,...
متن کاملmechanism-based studies of the active site-directed inhibition and activation of enzyme transketolase
derivatives of phenyl-keto butenoic acids have been reported to be inhibitors of pyruvate decarboxylase, (pdc). the inhibition of transketolase, a thiamine requiring enzyme such as pdf, by meta nitrophenyl derivative of 2-oxo-3-butenoic acid (mnpb) is reported here. these studies indicate that the inhibitor binds to the enzyme at the active site. a two-step inhibition was observed, first the in...
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ژورنال
عنوان ژورنال: Protein Engineering Design and Selection
سال: 1998
ISSN: 1741-0126,1741-0134
DOI: 10.1093/protein/11.12.1235