1pyn

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1pyn.gif|left|200px]]<br /><applet load="1pyn" size="350" color="white" frame="true" align="right" spinBox="true"
+
[[Image:1pyn.gif|left|200px]]
-
caption="1pyn, resolution 2.20&Aring;" />
+
 
-
'''DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE'''<br />
+
{{Structure
 +
|PDB= 1pyn |SIZE=350|CAPTION= <scene name='initialview01'>1pyn</scene>, resolution 2.20&Aring;
 +
|SITE=
 +
|LIGAND= <scene name='pdbligand=941:2-(4-{2-TERT-BUTOXYCARBONYLAMINO-2-[4-(3-HYDROXY-2-METHOXYCARBONYL-PHENOXY)-BUTYLCARBAMOYL]-ETHYL}-PHENOXY)-MALONIC ACID'>941</scene>
 +
|ACTIVITY= [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48]
 +
|GENE= PTPN1 OR PTP1B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
 +
}}
 +
 
 +
'''DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE'''
 +
 
==Overview==
==Overview==
Line 10: Line 19:
==About this Structure==
==About this Structure==
-
1PYN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=941:'>941</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1PYN OCA].
+
1PYN is a [[Single protein]] structure of 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=1PYN OCA].
==Reference==
==Reference==
-
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors., Pei Z, Li X, Liu G, Abad-Zapatero C, Lubben T, Zhang T, Ballaron SJ, Hutchins CW, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12951078 12951078]
+
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors., Pei Z, Li X, Liu G, Abad-Zapatero C, Lubben T, Zhang T, Ballaron SJ, Hutchins CW, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12951078 12951078]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein-tyrosine-phosphatase]]
[[Category: Protein-tyrosine-phosphatase]]
Line 31: Line 40:
[[Category: protein tyrosine phosphatase inhibited with dual site]]
[[Category: protein tyrosine phosphatase inhibited with dual site]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:33:56 2008''
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:30:41 2008''

Revision as of 11:30, 20 March 2008

Image:1pyn.gif


PDB ID 1pyn

Drag the structure with the mouse to rotate
, resolution 2.20Å
Ligands:
Gene: PTPN1 OR PTP1B (Homo sapiens)
Activity: Protein-tyrosine-phosphatase, with EC number 3.1.3.48
Coordinates: save as pdb, mmCIF, xml



DUAL-SITE POTENT, SELECTIVE PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR USING A LINKED FRAGMENT STRATEGY AND A MALONATE HEAD ON THE FIRST SITE


Contents

Overview

A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP.

Disease

Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]

About this Structure

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

Reference

Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors., Pei Z, Li X, Liu G, Abad-Zapatero C, Lubben T, Zhang T, Ballaron SJ, Hutchins CW, Trevillyan JM, Jirousek MR, Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32. PMID:12951078

Page seeded by OCA on Thu Mar 20 13:30:41 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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