1m4h: Difference between revisions

Line 1:

[[Image:1m4h.~~gif~~|left|200px]]

[[Image:1m4h.png|left|200px]]

<!--

Line 9:

Line 10:

~~'''~~Crystal Structure of Beta-secretase complexed with Inhibitor OM00-3~~'''~~

===Crystal Structure of Beta-secretase complexed with Inhibitor OM00-3===

~~==Overview==~~

<!--

The ~~structure of the catalytic domain of human memapsin 2 bound to an inhibitor OM00-3 (Glu-Leu-Asp-LeuAla-Val-Glu-Phe~~, ~~K(i) = 0.3 nM~~, the ~~asterisk denotes~~ the ~~hydroxyethylene transition-state isostere) has been determined~~ at 2.~~1 A resolution~~. ~~Uniquely defined in the structure are the locations of S(3~~)~~' and S(4)' subsites~~, ~~which were not identified in the previous structure of memapsin 2 in complex with~~ the ~~inhibitor OM99-2 (Glu-Val-Asn-LeuAla-Ala-Glu-Phe, K(i) = 1 nM)~~. Different binding modes for the P(2) and P(4) side chains are also observed. These new structural elements are useful for the design of new inhibitors. The structural and kinetic data indicate that the replacement of the P(2)' alanine in OM99-~~2 with a valine in OM00~~-~~3 stabilizes the binding of P(3)' and P(4)'.~~

The line below this paragraph, {{ABSTRACT_PUBMED_12206667}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 12206667 is the PubMed ID number.

-->

==About this Structure==

Line 34:

Line 38:

[[Category: Beta-secretase]]

[[Category: Memapsin2]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May~~ ~~3 00~~:37:10 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 23:11:25 2008''

Navigation menu

Page actions

Page actions

Personal tools

Navigation

Search

Tools

@@ Line 1: / Line 1: @@
-[[Image:1m4h.gif|left|200px]]
+{{Seed}}
+[[Image:1m4h.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_1m4h|  PDB=1m4h  |  SCENE=  }}
-'''Crystal Structure of Beta-secretase complexed with Inhibitor OM00-3'''
+===Crystal Structure of Beta-secretase complexed with Inhibitor OM00-3===
-==Overview==
+<!--
-The structure of the catalytic domain of human memapsin 2 bound to an inhibitor OM00-3 (Glu-Leu-Asp-LeuAla-Val-Glu-Phe, K(i) = 0.3 nM, the asterisk denotes the hydroxyethylene transition-state isostere) has been determined at 2.1 A resolution. Uniquely defined in the structure are the locations of S(3)' and S(4)' subsites, which were not identified in the previous structure of memapsin 2 in complex with the inhibitor OM99-2 (Glu-Val-Asn-LeuAla-Ala-Glu-Phe, K(i) = 1 nM). Different binding modes for the P(2) and P(4) side chains are also observed. These new structural elements are useful for the design of new inhibitors. The structural and kinetic data indicate that the replacement of the P(2)' alanine in OM99-2 with a valine in OM00-3 stabilizes the binding of P(3)' and P(4)'.
+The line below this paragraph, {{ABSTRACT_PUBMED_12206667}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 12206667 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_12206667}}
 ==About this Structure==
@@ Line 34: / Line 38: @@
 [[Category: Beta-secretase]]
 [[Category: Memapsin2]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 00:37:10 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul  2 23:11:25 2008''