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Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
Ala PJ, Gonneville L, Hillman MC, Becker-Pasha M, Wei M, Reid BG, Klabe R, Yue EW, Wayland B, Douty B, Polam P, Wasserman Z, Bower M, Combs AP, Burn TC, Hollis GF, Wynn R. Ala PJ, et al. Among authors: klabe r. J Biol Chem. 2006 Oct 27;281(43):32784-95. doi: 10.1074/jbc.M606873200. Epub 2006 Aug 17. J Biol Chem. 2006. PMID: 16916797 Free article.
Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.
Combs AP, Yue EW, Bower M, Ala PJ, Wayland B, Douty B, Takvorian A, Polam P, Wasserman Z, Zhu W, Crawley ML, Pruitt J, Sparks R, Glass B, Modi D, McLaughlin E, Bostrom L, Li M, Galya L, Blom K, Hillman M, Gonneville L, Reid BG, Wei M, Becker-Pasha M, Klabe R, Huber R, Li Y, Hollis G, Burn TC, Wynn R, Liu P, Metcalf B. Combs AP, et al. Among authors: klabe r. J Med Chem. 2005 Oct 20;48(21):6544-8. doi: 10.1021/jm0504555. J Med Chem. 2005. PMID: 16220970
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. Douty B, et al. Among authors: klabe r. Bioorg Med Chem Lett. 2008 Jan 1;18(1):66-71. doi: 10.1016/j.bmcl.2007.11.012. Epub 2007 Nov 9. Bioorg Med Chem Lett. 2008. PMID: 18037290
Phosphorylation State-Dependent High Throughput Screening of the c-Met Kinase.
Behshad E, Klabe RM, Margulis A, Becker-Pasha M, Rupar MJ, Collier P, Liu PC, Hollis GF, Burn TC, Wynn R. Behshad E, et al. Among authors: klabe rm. Curr Chem Genomics. 2010 Apr 23;4:27-33. doi: 10.2174/1875397301004010027. Curr Chem Genomics. 2010. PMID: 20556206 Free PMC article.
INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models.
Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G. Liu PCC, et al. Among authors: klabe r. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. PLoS One. 2020. PMID: 32315352 Free PMC article.
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Wu L, Zhang C, He C, Qian D, Lu L, Sun Y, Xu M, Zhuo J, Liu PCC, Klabe R, Wynn R, Covington M, Gallagher K, Leffet L, Bowman K, Diamond S, Koblish H, Zhang Y, Soloviev M, Hollis G, Burn TC, Scherle P, Yeleswaram S, Huber R, Yao W. Wu L, et al. Among authors: klabe r. J Med Chem. 2021 Aug 12;64(15):10666-10679. doi: 10.1021/acs.jmedchem.1c00713. Epub 2021 Jul 16. J Med Chem. 2021. PMID: 34269576
44 results