This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


1ym4

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1ym4.gif|left|200px]]
+
{{Seed}}
 +
[[Image:1ym4.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1ym4| PDB=1ym4 | SCENE= }}
{{STRUCTURE_1ym4| PDB=1ym4 | SCENE= }}
-
'''Crystal structure of human beta secretase complexed with NVP-AMK640'''
+
===Crystal structure of human beta secretase complexed with NVP-AMK640===
-
==Overview==
+
<!--
-
Molecular modeling based on the X-ray crystal structure of the Tang-Ghosh heptapeptide inhibitor 1 (OM99-2) of BACE led to the design and synthesis of a series of constrained P(1)' analogues. A cyclopentane ring was incorporated in 1 spanning the P(1)' Ala methyl group and the adjacent methylene carbon atom of the chain. Progressive truncation at the P(2)'-P(4)' sites led to a potent truncated analogue 5 with good selectivity over Cathepsin D. Using the same backbone replacement concept, a series of cyclopentane, cyclopentanone, tetrahydrofuran, pyrrolidine, and pyrrolidinone analogues were synthesized with considerable variation at the P and P' sites. The cyclopentanone and 2-pyrrolidinone analogues 45 and 57 showed low nM BACE inhibition. X-ray cocrystal structures of two analogues 5 and 45 revealed excellent convergence with the original inhibitor 1 structure while providing new insights into other interactions which could be exploited for future modifications.
+
The line below this paragraph, {{ABSTRACT_PUBMED_16078837}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 16078837 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_16078837}}
==About this Structure==
==About this Structure==
Line 36: Line 40:
[[Category: Beta-secretase]]
[[Category: Beta-secretase]]
[[Category: Memapsin2]]
[[Category: Memapsin2]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:29:56 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 01:12:28 2008''

Revision as of 22:12, 27 July 2008

Image:1ym4.png

Template:STRUCTURE 1ym4

Crystal structure of human beta secretase complexed with NVP-AMK640

Template:ABSTRACT PUBMED 16078837

About this Structure

1YM4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics., Hanessian S, Yun H, Hou Y, Yang G, Bayrakdarian M, Therrien E, Moitessier N, Roggo S, Veenstra S, Tintelnot-Blomley M, Rondeau JM, Ostermeier C, Strauss A, Ramage P, Paganetti P, Neumann U, Betschart C, J Med Chem. 2005 Aug 11;48(16):5175-90. PMID:16078837

Page seeded by OCA on Mon Jul 28 01:12:28 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1ym4"
Personal tools