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Literature DB >> 18680359

Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds.

Harshani R Lawrence¹, Roberta Pireddu, Liwei Chen, Yunting Luo, Shen-Shu Sung, Ann Marie Szymanski, M L Richard Yip, Wayne C Guida, Saïd M Sebti, Jie Wu, Nicholas J Lawrence.

Abstract

Screening of the NCI diversity set of compounds has led to the identification of 5 (NSC-117199), which inhibits the protein tyrosine phosphatase (PTP) Shp2 with an IC50 of 47 microM. A focused library incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to submicromolar activity. A model for the binding of the active compounds is proposed.

Entities: CellLine Chemical Disease Gene Species

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Year: 2008 PMID： 18680359 PMCID： PMC2744494 DOI： 10.1021/jm8002526

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

44 in total

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2. Stops along the RAS pathway in human genetic disease.

Authors: Mohamed Bentires-Alj; Maria I Kontaridis; Benjamin G Neel
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3. A common requirement for the catalytic activity and both SH2 domains of SHP-2 in mitogen-activated protein (MAP) kinase activation by the ErbB family of receptors. A specific role for SHP-2 in map, but not c-Jun amino-terminal kinase activation.

Authors: T B Deb; L Wong; D S Salomon; G Zhou; J E Dixon; J S Gutkind; S A Thompson; G R Johnson
Journal: J Biol Chem Date: 1998-07-03 Impact factor: 5.157

4. Both SH2 domains are involved in interaction of SHP-1 with the epidermal growth factor receptor but cannot confer receptor-directed activity to SHP-1/SHP-2 chimera.

Authors: T Tenev; H Keilhack; S Tomic; B Stoyanov; M Stein-Gerlach; R Lammers; A V Krivtsov; A Ullrich; F D Böhmer
Journal: J Biol Chem Date: 1997-02-28 Impact factor: 5.157

5. Crystal structure of the tyrosine phosphatase SHP-2.

Authors: P Hof; S Pluskey; S Dhe-Paganon; M J Eck; S E Shoelson
Journal: Cell Date: 1998-02-20 Impact factor: 41.582

6. Structural determinants of SHP-2 function and specificity in Xenopus mesoderm induction.

Authors: A M O'Reilly; B G Neel
Journal: Mol Cell Biol Date: 1998-01 Impact factor: 4.272

7. Protein tyrosine phosphatases in signal transduction.

Authors: B G Neel; N K Tonks
Journal: Curr Opin Cell Biol Date: 1997-04 Impact factor: 8.382

8. The NCI Drug Information System. 2. DIS Pre-Registry.

Authors: G W Milne; A Feldman; J A Miller; G P Daly; M J Hammel
Journal: J Chem Inf Comput Sci Date: 1986-11

Review 9. Targeting the PTPome in human disease.

Authors: Lutz Tautz; Maurizio Pellecchia; Tomas Mustelin
Journal: Expert Opin Ther Targets Date: 2006-02 Impact factor: 6.902

Review 10. Protein tyrosine phosphatases in the human genome.

Authors: Andres Alonso; Joanna Sasin; Nunzio Bottini; Ilan Friedberg; Iddo Friedberg; Andrei Osterman; Adam Godzik; Tony Hunter; Jack Dixon; Tomas Mustelin
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22 in total

1. Enhanced anti-melanoma efficacy of interferon alfa-2b via inhibition of Shp2.

Authors: Hla Win-Piazza; Valentina E Schneeberger; Liwei Chen; Daniele Pernazza; Harshani R Lawrence; Said M Sebti; Nicholas J Lawrence; Jie Wu
Journal: Cancer Lett Date: 2012-02-01 Impact factor: 8.679

2. Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2).

Authors: Xian Zhang; Yantao He; Sijiu Liu; Zhihong Yu; Zhong-Xing Jiang; Zhenyun Yang; Yuanshu Dong; Sarah C Nabinger; Li Wu; Andrea M Gunawan; Lina Wang; Rebecca J Chan; Zhong-Yin Zhang
Journal: J Med Chem Date: 2010-03-25 Impact factor: 7.446

Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds.

Review 1. The role of Gab family scaffolding adapter proteins in the signal transduction of cytokine and growth factor receptors.

2. Stops along the RAS pathway in human genetic disease.

3. A common requirement for the catalytic activity and both SH2 domains of SHP-2 in mitogen-activated protein (MAP) kinase activation by the ErbB family of receptors. A specific role for SHP-2 in map, but not c-Jun amino-terminal kinase activation.

4. Both SH2 domains are involved in interaction of SHP-1 with the epidermal growth factor receptor but cannot confer receptor-directed activity to SHP-1/SHP-2 chimera.

5. Crystal structure of the tyrosine phosphatase SHP-2.

6. Structural determinants of SHP-2 function and specificity in Xenopus mesoderm induction.

7. Protein tyrosine phosphatases in signal transduction.

8. The NCI Drug Information System. 2. DIS Pre-Registry.

Review 9. Targeting the PTPome in human disease.

Review 10. Protein tyrosine phosphatases in the human genome.

1. Enhanced anti-melanoma efficacy of interferon alfa-2b via inhibition of Shp2.

2. Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2).

Review 3. Targeting protein tyrosine phosphatases for anticancer drug discovery.

Review 4. Small molecule tools for functional interrogation of protein tyrosine phosphatases.

Review 5. Phosphotyrosine isosteres: past, present and future.

6. Small molecule inhibitors of SHP2 tyrosine phosphatase discovered by virtual screening.

7. Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.

8. Structure based design of selective SHP2 inhibitors by De novo design, synthesis and biological evaluation.

9. Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2.

Review 10. Protein tyrosine phosphatases: structure, function, and implication in human disease.