2vex
| |||||||
| , resolution 2.2Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | and | ||||||
| Ligands: | and | ||||||
| Activity: | Protein-tyrosine-phosphatase, with EC number 3.1.3.48 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
CRYSTAL STRUCUTRE OF PROTEIN TYROSINE PHOSPHATASE 1B IN COMPLEX WITH AN ISOTHIAZOLIDINONE-CONTAINING INHIBITOR
OverviewOverview
The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.
DiseaseDisease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this StructureAbout this Structure
2VEX is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines., Douty B, Wayland B, Ala PJ, Bower MJ, Pruitt J, Bostrom L, Wei M, Klabe R, Gonneville L, Wynn R, Burn TC, Liu PC, Combs AP, Yue EW, Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. Epub 2007 Nov 9. PMID:18037290
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- Homo sapiens
- Protein-tyrosine-phosphatase
- Single protein
- Ala, P J.
- Bostrom, L.
- Bower, M J.
- Burn, T C.
- Combs, A P.
- Douty, B.
- Gonneville, L.
- Klabe, R.
- Liu, P C.C.
- Pruitt, J.
- Wayland, B.
- Wei, M.
- Wynn, R.
- Yue, E W.
- IZ4
- MG
- Acetylation
- Endoplasmic reticulum
- Hydrolase
- Membrane
- Oxidation
- Phosphatase
- Phosphorylation
- Polymorphism
- Protein phosphatase