10kz: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
==N-Alkyl & N-Aryl Aminopyrazole Spirocarbamates: A Two-Pronged Lead Optimization Strategy to Identify Orally Bioavailable Plasma Kallikrein Inhibitors== | |||
<StructureSection load='10kz' size='340' side='right'caption='[[10kz]], [[Resolution|resolution]] 1.78Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[10kz]] is a 1 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=10KZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=10KZ 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]] 1.78Å</td></tr> | |||
[[Category: | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1C6O:(3R)-1-(1-benzyl-1H-pyrazole-4-carbonyl)-6-chloro-5-fluorospiro[[3,1]benzoxazine-4,3-piperidin]-2(1H)-one'>A1C6O</scene></td></tr> | ||
[[Category: | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=10kz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=10kz OCA], [https://pdbe.org/10kz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=10kz RCSB], [https://www.ebi.ac.uk/pdbsum/10kz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=10kz ProSAT]</span></td></tr> | ||
[[Category: | </table> | ||
[[Category: | == Disease == | ||
[[Category: | [https://www.uniprot.org/uniprot/KLKB1_HUMAN KLKB1_HUMAN] Defects in KLKB1 are the cause of prekallikrein deficiency (PKK deficiency) [MIM:[https://omim.org/entry/612423 612423]; also known as Fletcher factor deficiency. This disorder is a blood coagulation defect. | ||
[[Category: Fier | == Function == | ||
[[Category: | [https://www.uniprot.org/uniprot/KLKB1_HUMAN KLKB1_HUMAN] The enzyme cleaves Lys-Arg and Arg-Ser bonds. It activates, in a reciprocal reaction, factor XII after its binding to a negatively charged surface. It also releases bradykinin from HMW kininogen and may also play a role in the renin-angiotensin system by converting prorenin into renin. | ||
[[Category: | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: | [[Category: Cheng A]] | ||
[[Category: | [[Category: Chernyak N]] | ||
[[Category: | [[Category: Ellsworth K]] | ||
[[Category: | [[Category: Esmay J]] | ||
[[Category: | [[Category: Fier P]] | ||
[[Category: | [[Category: He J]] | ||
[[Category: | [[Category: Hicks J]] | ||
[[Category: | [[Category: Hruza A]] | ||
[[Category: | [[Category: Lin K]] | ||
[[Category: Lopez JA]] | |||
[[Category: Mandal M]] | |||
[[Category: Merchant RR]] | |||
[[Category: Ogawa A]] | |||
[[Category: Piou T]] | |||
[[Category: Rearden P]] | |||
[[Category: Sharp PP]] | |||
[[Category: Sinz C]] | |||
[[Category: Tatosian DA]] | |||
[[Category: Yang S]] | |||
Latest revision as of 08:50, 11 March 2026
N-Alkyl & N-Aryl Aminopyrazole Spirocarbamates: A Two-Pronged Lead Optimization Strategy to Identify Orally Bioavailable Plasma Kallikrein Inhibitors
| ||||||||||||
