2qpj: Difference between revisions

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==Overview==

Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic, inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor, as well, as the incretin hormone glucagon-like peptide 1 (GLP-1), which is a potent, stimulator of insulin secretion. The activity of GLP-1 is also rapidly, abolished by the serine protease dipeptidyl peptidase IV (DPP-IV), which, led to an elevated interest in inhibitors of this enzyme for the treatment, of type II diabetes. A dual NEP/DPP-IV inhibitor concept is proposed, offering an alternative strategy for the treatment of type 2 diabetes., Here, the synthesis and crystal structures of the soluble extracellular, domain of human NEP (residues 52-749) complexed with the NEP, competitive, and potent dual NEP/DPP-IV inhibitor MCB3937 are described.

Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor, as well as the incretin hormone glucagon-like peptide 1 (GLP-1), which is a potent stimulator of insulin secretion. The activity of GLP-1 is also rapidly abolished by the serine protease dipeptidyl peptidase IV (DPP-IV), which led to an elevated interest in inhibitors of this enzyme for the treatment of type II diabetes. A dual NEP/DPP-IV inhibitor concept is proposed, offering an alternative strategy for the treatment of type 2 diabetes. Here, the synthesis and crystal structures of the soluble extracellular domain of human NEP (residues 52-749) complexed with the NEP, competitive and potent dual NEP/DPP-IV inhibitor MCB3937 are described.

==About this Structure==

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[[Category: Neprilysin]]

[[Category: Single protein]]

[[Category: Dale, G.E.]]

[[Category: Dale, G E.]]

[[Category: Oefner, C.]]

[[Category: I20]]

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[[Category: zinc-dependent metalloprotease]]

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@@ Line 4: / Line 4: @@
 ==Overview==
-Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic, inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor, as well, as the incretin hormone glucagon-like peptide 1 (GLP-1), which is a potent, stimulator of insulin secretion. The activity of GLP-1 is also rapidly, abolished by the serine protease dipeptidyl peptidase IV (DPP-IV), which, led to an elevated interest in inhibitors of this enzyme for the treatment, of type II diabetes. A dual NEP/DPP-IV inhibitor concept is proposed, offering an alternative strategy for the treatment of type 2 diabetes., Here, the synthesis and crystal structures of the soluble extracellular, domain of human NEP (residues 52-749) complexed with the NEP, competitive, and potent dual NEP/DPP-IV inhibitor MCB3937 are described.
+Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor, as well as the incretin hormone glucagon-like peptide 1 (GLP-1), which is a potent stimulator of insulin secretion. The activity of GLP-1 is also rapidly abolished by the serine protease dipeptidyl peptidase IV (DPP-IV), which led to an elevated interest in inhibitors of this enzyme for the treatment of type II diabetes. A dual NEP/DPP-IV inhibitor concept is proposed, offering an alternative strategy for the treatment of type 2 diabetes. Here, the synthesis and crystal structures of the soluble extracellular domain of human NEP (residues 52-749) complexed with the NEP, competitive and potent dual NEP/DPP-IV inhibitor MCB3937 are described.
 ==About this Structure==
@@ Line 14: / Line 14: @@
 [[Category: Neprilysin]]
 [[Category: Single protein]]
-[[Category: Dale, G.E.]]
+[[Category: Dale, G E.]]
 [[Category: Oefner, C.]]
 [[Category: I20]]
@@ Line 28: / Line 28: @@
 [[Category: zinc-dependent metalloprotease]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 11:59:17 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:41:10 2008''