1onz

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
m (Protected "1onz" [edit=sysop:move=sysop])
Current revision (09:29, 16 August 2023) (edit) (undo)
 
(8 intermediate revisions not shown.)
Line 1: Line 1:
-
[[Image:1onz.png|left|200px]]
 
-
{{STRUCTURE_1onz| PDB=1onz | SCENE= }}
+
==Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b==
 +
<StructureSection load='1onz' size='340' side='right'caption='[[1onz]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[1onz]] 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=1ONZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1ONZ 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]] 2.4&#8491;</td></tr>
 +
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=968:2-[(7-HYDROXY-NAPHTHALEN-1-YL)-OXALYL-AMINO]-BENZOIC+ACID'>968</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=1onz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1onz OCA], [https://pdbe.org/1onz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1onz RCSB], [https://www.ebi.ac.uk/pdbsum/1onz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1onz ProSAT]</span></td></tr>
 +
</table>
 +
== Function ==
 +
[https://www.uniprot.org/uniprot/PTN1_HUMAN PTN1_HUMAN] Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion.<ref>PMID:21135139</ref> <ref>PMID:22169477</ref>
 +
== Evolutionary Conservation ==
 +
[[Image:Consurf_key_small.gif|200px|right]]
 +
Check<jmol>
 +
<jmolCheckbox>
 +
<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/on/1onz_consurf.spt"</scriptWhenChecked>
 +
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
 +
<text>to colour the structure by Evolutionary Conservation</text>
 +
</jmolCheckbox>
 +
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1onz ConSurf].
 +
<div style="clear:both"></div>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
Protein Tyrosine phosphatase 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling pathways. Using an NMR-based screening approach with 15N- and 13C-labeled PTP1B, we have identified 2,3-dimethylphenyloxalylaminobenzoic acid (1) as a general, reversible, and competitive PTPase inhibitor. Structure-based approach guided by X-ray crystallography facilitated the development of 1 into a novel series of potent and selective PTP1B inhibitors occupying both the catalytic site and a portion of the noncatalytic, second phosphotyrosine binding site. Interestingly, oral biovailability has been observed in rats for some compounds. Furthermore, we demonstrated in vivo plasma glucose lowering effects with compound 12d in ob/ob mice.
-
===Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b===
+
Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.,Liu G, Szczepankiewicz BG, Pei Z, Janowick DA, Xin Z, Hajduk PJ, Abad-Zapatero C, Liang H, Hutchins CW, Fesik SW, Ballaron SJ, Stashko MA, Lubben T, Mika AK, Zinker BA, Trevillyan JM, Jirousek MR J Med Chem. 2003 May 22;46(11):2093-103. PMID:12747781<ref>PMID:12747781</ref>
-
{{ABSTRACT_PUBMED_12747781}}
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
 
+
</div>
-
==About this Structure==
+
<div class="pdbe-citations 1onz" style="background-color:#fffaf0;"></div>
-
[[1onz]] is a 1 chain structure of [[Proten tyrosine phosphatase]] and [[Tyrosine phosphatase]] 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=1ONZ OCA].
+
==See Also==
==See Also==
-
*[[Proten tyrosine phosphatase|Proten tyrosine phosphatase]]
+
*[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]]
-
*[[Tyrosine phosphatase|Tyrosine phosphatase]]
+
== References ==
-
 
+
<references/>
-
==Reference==
+
__TOC__
-
<ref group="xtra">PMID:012747781</ref><ref group="xtra">PMID:015258570</ref><references group="xtra"/>
+
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Protein-tyrosine-phosphatase]]
+
[[Category: Large Structures]]
-
[[Category: Abad-Zapatero, C.]]
+
[[Category: Abad-Zapatero C]]
-
[[Category: Ballaron, S J.]]
+
[[Category: Ballaron SJ]]
-
[[Category: Fesik, S W.]]
+
[[Category: Fesik SW]]
-
[[Category: Hadjuk, P J.]]
+
[[Category: Hadjuk PJ]]
-
[[Category: Hutchins, C W.]]
+
[[Category: Hutchins CW]]
-
[[Category: Janowich, D A.]]
+
[[Category: Janowich DA]]
-
[[Category: Jirousek, M R.]]
+
[[Category: Jirousek MR]]
-
[[Category: Liang, H.]]
+
[[Category: Liang H]]
-
[[Category: Liu, G.]]
+
[[Category: Liu G]]
-
[[Category: Lubben, T.]]
+
[[Category: Lubben T]]
-
[[Category: Mika, A K.]]
+
[[Category: Mika AK]]
-
[[Category: Pei, Z.]]
+
[[Category: Pei Z]]
-
[[Category: Stashko, M A.]]
+
[[Category: Stashko MA]]
-
[[Category: Szczepankiewicz, B G.]]
+
[[Category: Szczepankiewicz BG]]
-
[[Category: Trevillyan, J M.]]
+
[[Category: Trevillyan JM]]
-
[[Category: Xin, Z.]]
+
[[Category: Xin Z]]
-
[[Category: Zinker, B A.]]
+
[[Category: Zinker BA]]
-
[[Category: Hydrolase]]
+
-
[[Category: Oxalyl-aryl-benzoic acid compound with napthyl moiety anchor inhibitor]]
+
-
[[Category: Protein tyrosine phosphatase]]
+

Current revision

Oxalyl-aryl-Amino Benzoic acid Inhibitors of PTP1B, compound 8b

PDB ID 1onz

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/1onz"
Personal tools