1sl3: Difference between revisions

← Older edit Newer edit →

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

@@ Line 1: / Line 1: @@
-[[Image:1sl3.jpg|left|200px]]
+{{Seed}}
+[[Image:1sl3.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_1sl3|  PDB=1sl3  |  SCENE=  }}
-'''crystal structue of Thrombin in complex with a potent P1 heterocycle-Aryl based inhibitor'''
+===crystal structue of Thrombin in complex with a potent P1 heterocycle-Aryl based inhibitor===
-==Overview==
+<!--
-In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic approach was used to explore the P(1) region. Various benzylamines were coupled to a pyridine/pyrazinone P(2)-P(3) template. One compound with an o-thiadiazole benzylic substitution was found to have a thrombin K(i) of 0.84 nM. A study of ortho-substituted five-membered-ring heterocycles was undertaken and subsequently demonstrated that the o-triazole and tetrazole rings were optimal. Combination of these potent P(1) aryl heterocycles with a variety of P(2)-P(3) groups produced a compound with an extraordinary thrombin inhibitory activity of 1.4 pM. It is hoped that this potency enhancement in P(1) will allow for more diversification in the P(2)-P(3) region to ultimately address additional pharmacological concerns.
+The line below this paragraph, {{ABSTRACT_PUBMED_15163182}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 15163182 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_15163182}}
 ==About this Structure==
@@ Line 45: / Line 49: @@
 [[Category: Young, M B.]]
 [[Category: Thrombin inhibitor complex]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 08:50:20 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 16:09:16 2008''