2y7x

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (08:09, 23 August 2023) (edit) (undo)
 
(6 intermediate revisions not shown.)
Line 1: Line 1:
-
{{STRUCTURE_2y7x| PDB=2y7x | SCENE= }}
 
-
===THE DISCOVERY OF POTENT AND LONG-ACTING ORAL FACTOR XA INHIBITORS WITH TETRAHYDROISOQUINOLINE AND BENZAZEPINE P4 MOTIFS===
 
-
{{ABSTRACT_PUBMED_21349711}}
 
-
==Disease==
+
==The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs==
-
[[http://www.uniprot.org/uniprot/FA10_HUMAN FA10_HUMAN]] Defects in F10 are the cause of factor X deficiency (FA10D) [MIM:[http://omim.org/entry/227600 227600]]. A hemorrhagic disease with variable presentation. Affected individuals can manifest prolonged nasal and mucosal hemorrhage, menorrhagia, hematuria, and occasionally hemarthrosis. Some patients do not have clinical bleeding diathesis.<ref>PMID:2790181</ref><ref>PMID:1973167</ref><ref>PMID:1985698</ref><ref>PMID:7669671</ref><ref>PMID:8529633</ref><ref>PMID:7860069</ref><ref>PMID:8845463</ref><ref>PMID:8910490</ref><ref>PMID:10468877</ref><ref>PMID:10746568</ref><ref>PMID:10739379</ref><ref>PMID:11248282</ref><ref>PMID:11728527</ref><ref>PMID:12945883</ref><ref>PMID:15650540</ref><ref>PMID:17393015</ref><ref>PMID:19135706</ref>
+
<StructureSection load='2y7x' size='340' side='right'caption='[[2y7x]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[2y7x]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y7X OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Y7X FirstGlance]. <br>
 +
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.9&#8491;</td></tr>
 +
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=MZA:6-CHLORO-N-[(3S)-1-(5-FLUORO-1,2,3,4-TETRAHYDROISOQUINOLIN-6-YL)-2-OXO-PYRROLIDIN-3-YL]NAPHTHALENE-2-SULFONAMIDE'>MZA</scene></td></tr>
 +
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2y7x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y7x OCA], [https://pdbe.org/2y7x PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2y7x RCSB], [https://www.ebi.ac.uk/pdbsum/2y7x PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2y7x ProSAT]</span></td></tr>
 +
</table>
 +
== Disease ==
 +
[https://www.uniprot.org/uniprot/FA10_HUMAN FA10_HUMAN] Defects in F10 are the cause of factor X deficiency (FA10D) [MIM:[https://omim.org/entry/227600 227600]. A hemorrhagic disease with variable presentation. Affected individuals can manifest prolonged nasal and mucosal hemorrhage, menorrhagia, hematuria, and occasionally hemarthrosis. Some patients do not have clinical bleeding diathesis.<ref>PMID:2790181</ref> <ref>PMID:1973167</ref> <ref>PMID:1985698</ref> <ref>PMID:7669671</ref> <ref>PMID:8529633</ref> <ref>PMID:7860069</ref> <ref>PMID:8845463</ref> <ref>PMID:8910490</ref> <ref>PMID:10468877</ref> <ref>PMID:10746568</ref> <ref>PMID:10739379</ref> <ref>PMID:11248282</ref> <ref>PMID:11728527</ref> <ref>PMID:12945883</ref> <ref>PMID:15650540</ref> <ref>PMID:17393015</ref> <ref>PMID:19135706</ref>
 +
== Function ==
 +
[https://www.uniprot.org/uniprot/FA10_HUMAN FA10_HUMAN] Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the former series were addressed in the later, delivering a robust candidate for progression towards clinical studies.
-
==Function==
+
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.,Watson NS, Adams C, Belton D, Brown D, Burns-Kurtis CL, Chaudry L, Chan C, Convery MA, Davies DE, Exall AM, Harling JD, Irvine S, Irving WR, Kleanthous S, McLay IM, Pateman AJ, Patikis AN, Roethke TJ, Senger S, Stelman GJ, Toomey JR, West RI, Whittaker C, Zhou P, Young RJ Bioorg Med Chem Lett. 2011 Mar 15;21(6):1588-92. Epub 2011 Feb 2. PMID:21349711<ref>PMID:21349711</ref>
-
[[http://www.uniprot.org/uniprot/FA10_HUMAN FA10_HUMAN]] Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
+
-
==About this Structure==
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
[[2y7x]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y7X OCA].
+
</div>
 +
<div class="pdbe-citations 2y7x" style="background-color:#fffaf0;"></div>
==See Also==
==See Also==
*[[Factor Xa|Factor Xa]]
*[[Factor Xa|Factor Xa]]
-
 
+
== References ==
-
==Reference==
+
<references/>
-
<ref group="xtra">PMID:021349711</ref><references group="xtra"/><references/>
+
__TOC__
-
[[Category: Coagulation factor Xa]]
+
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Adams, C.]]
+
[[Category: Large Structures]]
-
[[Category: Belton, D.]]
+
[[Category: Adams C]]
-
[[Category: Brown, D.]]
+
[[Category: Belton D]]
-
[[Category: Burns-Kurtis, C L.]]
+
[[Category: Brown D]]
-
[[Category: Chan, C.]]
+
[[Category: Burns-Kurtis CL]]
-
[[Category: Chaudry, L.]]
+
[[Category: Chan C]]
-
[[Category: Convery, M A.]]
+
[[Category: Chaudry L]]
-
[[Category: Davies, D E.]]
+
[[Category: Convery MA]]
-
[[Category: Exall, A M.]]
+
[[Category: Davies DE]]
-
[[Category: Harling, J D.]]
+
[[Category: Exall AM]]
-
[[Category: Irvine, S.]]
+
[[Category: Harling JD]]
-
[[Category: Irving, W R.]]
+
[[Category: Irvine S]]
-
[[Category: Kleanthous, S.]]
+
[[Category: Irving WR]]
-
[[Category: Mclay, I M.]]
+
[[Category: Kleanthous S]]
-
[[Category: Pateman, A J.]]
+
[[Category: McLay IM]]
-
[[Category: Patikis, A N.]]
+
[[Category: Pateman AJ]]
-
[[Category: Roethka, T J.]]
+
[[Category: Patikis AN]]
-
[[Category: Senger, S.]]
+
[[Category: Roethka TJ]]
-
[[Category: Stelman, G J.]]
+
[[Category: Senger S]]
-
[[Category: Toomey, J R.]]
+
[[Category: Stelman GJ]]
-
[[Category: Watson, N S.]]
+
[[Category: Toomey JR]]
-
[[Category: West, R I.]]
+
[[Category: Watson NS]]
-
[[Category: Whittaker, C.]]
+
[[Category: West RI]]
-
[[Category: Young, R J.]]
+
[[Category: Whittaker C]]
-
[[Category: Zhou, P.]]
+
[[Category: Young RJ]]
-
[[Category: Blood clotting]]
+
[[Category: Zhou P]]
-
[[Category: Hydrolase]]
+
-
[[Category: Serine protease]]
+

Current revision

The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs

PDB ID 2y7x

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2y7x"
Personal tools