2f6t: Difference between revisions

Revision as of 03:32, 4 May 2008

Protein tyrosine phosphatase 1B with sulfamic acid inhibitors

OverviewOverview

High-throughput screening of the P&GP corporate repository against several protein tyrosine phosphatases identified the sulfamic acid moiety as potential phosphotyrosine mimetic. Incorporation of the sulfamic acid onto a 1,2,3,4-tetrahydroisoquinoline scaffold provided a promising starting point for PTP1B inhibitor design.

About this StructureAbout this Structure

2F6T is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

1,2,3,4-Tetrahydroisoquinolinyl sulfamic acids as phosphatase PTP1B inhibitors., Klopfenstein SR, Evdokimov AG, Colson AO, Fairweather NT, Neuman JJ, Maier MB, Gray JL, Gerwe GS, Stake GE, Howard BW, Farmer JA, Pokross ME, Downs TR, Kasibhatla B, Peters KG, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1574-8. Epub 2006 Jan 4. PMID:16386905 Page seeded by OCA on Sun May 4 03:31:59 2008

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

OCA

@@ Line 1: / Line 1: @@
 [[Image:2f6t.gif|left|200px]]
- {{Structure
+<!--
-|PDB= 2f6t |SIZE=350|CAPTION= <scene name='initialview01'>2f6t</scene>, resolution 1.700&Aring;
+The line below this paragraph, containing "STRUCTURE_2f6t", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=1C2:3(S)-METHYLCARBAMOYL-7-SULFOAMINO-3,4-DIHYDRO-1H-ISOQUINOLINE-2-CARBOXYLIC+ACID+TERT-BUTYL+ESTER'>1C2</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY= <span class='plainlinks'>[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] </span>
+or leave the SCENE parameter empty for the default display.
-|GENE= PTPN1, PTP1B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+-->
-|DOMAIN=
+{{STRUCTURE_2f6t|  PDB=2f6t  |  SCENE=  }}
-|RELATEDENTRY=[[2f6v|2F6V]], [[2f6w|2F6W]], [[2f6y|2F6Y]], [[2f6z|2F6Z]], [[2f70|2F70]], [[2f71|2F71]]
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2f6t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2f6t OCA], [http://www.ebi.ac.uk/pdbsum/2f6t PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2f6t RCSB]</span>
-}}
 '''Protein tyrosine phosphatase 1B with sulfamic acid inhibitors'''
@@ Line 29: / Line 26: @@
 [[Category: Klopfenstein, S R.]]
 [[Category: Pokross, M E.]]
-[[Category: phosphatase]]
+[[Category: Phosphatase]]
-[[Category: ptp1b]]
+[[Category: Ptp1b]]
-[[Category: sulfamic acid]]
+[[Category: Sulfamic acid]]
-[[Category: tetrahydroisoquinoline]]
+[[Category: Tetrahydroisoquinoline]]
-[[Category: tyrosine]]
+[[Category: Tyrosine]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 03:31:59 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:58:41 2008''