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The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay.

Tecle H, Feru F, Liu H, Kuhn C, Rennie G, Morris M, Shao J, Cheng AC, Gikunju D, Miret J, Coli R, Xi SH, Clugston SL, Low S, Kazmirski S, Ding YH, Cao Q, Johnson TL, Deshmukh GD, DiNitto JP, Wu JC, English JM
Chem Biol Drug Des 74 547-59 (2009)
Cited: 6 times
EuropePMC logo PMID: 19843080

Abstract

The design, synthesis and utility of fluorescence probes that bind to the DFG-out conformation of p38alpha kinase are described. Probes that demonstrate good affinity for p38alpha, have been identified and one of the probes, PF-04438255, has been successfully used in an high throughput screening (HTS) assay to identify two novel non-classical p38alpha inhibitors. In addition, a cascade activity assay was utilized to validate the selective binding of these non-classical kinase inhibitors to the unactive form of the enzyme.

Articles - 3k3j mentioned but not cited (2)

  1. Structural basis of a redox-dependent conformational switch that regulates the stress kinase p38α. Pous J, Baginski B, Martin-Malpartida P, González L, Scarpa M, Aragon E, Ruiz L, Mees RA, Iglesias-Fernández J, Orozco M, Nebreda AR, Macias MJ. Nat Commun 14 7920 (2023)
  2. p38α Mitogen-Activated Protein Kinase Is a Druggable Target in Pancreatic Adenocarcinoma. Yang L, Sun X, Ye Y, Lu Y, Zuo J, Liu W, Elcock A, Zhu S. Front Oncol 9 1294 (2019)


Reviews citing this publication (1)

  1. Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? Zhao Z, Wu H, Wang L, Liu Y, Knapp S, Liu Q, Gray NS. ACS Chem. Biol. 9 1230-1241 (2014)

Articles citing this publication (3)

  1. Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. Cowan-Jacob SW, Jahnke W, Knapp S. Future Med Chem 6 541-561 (2014)
  2. Identification of type-II inhibitors using kinase structures. Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A. Chem Biol Drug Des 80 657-664 (2012)
  3. Next-Generation JAK2 Inhibitors for the Treatment of Myeloproliferative Neoplasms: Lessons from Structure-Based Drug Discovery Approaches. Nair PC, Piehler J, Tvorogov D, Ross DM, Lopez AF, Gotlib J, Thomas D. Blood Cancer Discov 4 352-364 (2023)


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