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Engineering the catalytic domain of human protein tyrosine phosphatase beta for structure-based drug discovery.

Evdokimov AG, Pokross M, Walter R, Mekel M, Cox B, Li C, Bechard R, Genbauffe F, Andrews R, Diven C, Howard B, Rastogi V, Gray J, Maier M, Peters KG
Acta Crystallogr D Biol Crystallogr 62 1435-45 (2006)
Related entries: 2hc2, 2i3r, 2i3u, 2i4e, 2i4g, 2i4h, 2i5x

Cited: 14 times
EuropePMC logo PMID: 17139078

Abstract

Protein tyrosine phosphatases (PTPs) play roles in many biological processes and are considered to be important targets for drug discovery. As inhibitor development has proven challenging, crystal structure-based design will be very helpful to advance inhibitor potency and selectivity. Successful application of protein crystallography to drug discovery heavily relies on high-quality crystal structures of the protein of interest complexed with pharmaceutically interesting ligands. It is very important to be able to produce protein-ligand crystals rapidly and reproducibly for as many ligands as necessary. This study details our efforts to engineer the catalytic domain of human protein tyrosine phosphatase beta (HPTPbeta-CD) with properties suitable for rapid-turnaround crystallography. Structures of apo HPTPbeta-CD and its complexes with several novel small-molecule inhibitors are presented here for the first time.

Articles - 2hc1 mentioned but not cited (2)

  1. Using iterative fragment assembly and progressive sequence truncation to facilitate phasing and crystal structure determination of distantly related proteins. Wang Y, Virtanen J, Xue Z, Tesmer JJ, Zhang Y. Acta Crystallogr D Struct Biol 72 616-628 (2016)
  2. The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. Chakraborty S, Rendón-Ramírez A, Ásgeirsson B, Dutta M, Ghosh AS, Oda M, Venkatramani R, Rao BJ, Dandekar AM, Goñi FM. F1000Res 2 286 (2013)


Reviews citing this publication (2)

  1. Protein tyrosine phosphatases: structure-function relationships. Tabernero L, Aricescu AR, Jones EY, Szedlacsek SE. FEBS J 275 867-882 (2008)
  2. Vanadium in Biological Action: Chemical, Pharmacological Aspects, and Metabolic Implications in Diabetes Mellitus. Treviño S, Díaz A, Sánchez-Lara E, Sanchez-Gaytan BL, Perez-Aguilar JM, González-Vergara E. Biol Trace Elem Res 188 68-98 (2019)

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  1. Targeting VE-PTP activates TIE2 and stabilizes the ocular vasculature. Shen J, Frye M, Lee BL, Reinardy JL, McClung JM, Ding K, Kojima M, Xia H, Seidel C, Lima e Silva R, Dong A, Hackett SF, Wang J, Howard BW, Vestweber D, Kontos CD, Peters KG, Campochiaro PA. J Clin Invest 124 4564-4576 (2014)
  2. Picomolar concentrations of free zinc(II) ions regulate receptor protein-tyrosine phosphatase β activity. Wilson M, Hogstrand C, Maret W. J Biol Chem 287 9322-9326 (2012)
  3. Insights into the reaction of protein-tyrosine phosphatase 1B: crystal structures for transition state analogs of both catalytic steps. Brandão TA, Hengge AC, Johnson SJ. J Biol Chem 285 15874-15883 (2010)
  4. The Search for Herbal Antibiotics: An In-Silico Investigation of Antibacterial Phytochemicals. Snow Setzer M, Sharifi-Rad J, Setzer WN. Antibiotics (Basel) 5 E30 (2016)
  5. Infection-Induced Vascular Permeability Aids Mycobacterial Growth. Oehlers SH, Cronan MR, Beerman RW, Johnson MG, Huang J, Kontos CD, Stout JE, Tobin DM. J Infect Dis 215 813-817 (2017)
  6. Visualizing active-site dynamics in single crystals of HePTP: opening of the WPD loop involves coordinated movement of the E loop. Critton DA, Tautz L, Page R. J Mol Biol 405 619-629 (2011)
  7. Unscrambling the effect of C-terminal tail deletion on the stability of a cold-adapted, organic solvent stable lipase from Staphylococcus epidermidis AT2. Kamarudin NH, Rahman RN, Ali MS, Leow TC, Basri M, Salleh AB. Mol Biotechnol 56 747-757 (2014)
  8. Evaluating transition state structures of vanadium-phosphatase protein complexes using shape analysis. Sánchez-Lombardo I, Alvarez S, McLauchlan CC, Crans DC. J Inorg Biochem 147 153-164 (2015)
  9. Rational protein engineering in action: the first crystal structure of a phenylalanine tRNA synthetase from Staphylococcus haemolyticus. Evdokimov AG, Mekel M, Hutchings K, Narasimhan L, Holler T, McGrath T, Beattie B, Fauman E, Yan C, Heaslet H, Walter R, Finzel B, Ohren J, McConnell P, Braden T, Sun F, Spessard C, Banotai C, Al-Kassim L, Ma W, Wengender P, Kole D, Garceau N, Toogood P, Liu J. J Struct Biol 162 152-169 (2008)
  10. Crystal structure of the catalytic domain of human RPTPH. Kim M, Ryu SE. Acta Crystallogr F Struct Biol Commun 78 265-269 (2022)


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