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The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.

Lucet IS, Fantino E, Styles M, Bamert R, Patel O, Broughton SE, Walter M, Burns CJ, Treutlein H, Wilks AF, Rossjohn J
Blood 107 176-83 (2006)
Cited: 174 times
EuropePMC logo PMID: 16174768

Abstract

JAK2, a member of the Janus kinase (JAK) family of protein tyrosine kinases (PTKs), is an important intracellular mediator of cytokine signaling. Mutations of the JAK2 gene are associated with hematologic cancers, and aberrant JAK activity is also associated with a number of immune diseases, including rheumatoid arthritis. Accordingly, the development of JAK2-specific inhibitors has tremendous clinical relevance. Critical to the function of JAK2 is its PTK domain. We report the 2.0 A crystal structure of the active conformation of the JAK2 PTK domain in complex with a high-affinity, pan-JAK inhibitor that appears to bind via an induced fit mechanism. This inhibitor, the tetracyclic pyridone 2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-1, was buried deep within a constricted ATP-binding site, in which extensive interactions, including residues that are unique to JAK2 and the JAK family, are made with the inhibitor. We present a structural basis of high-affinity JAK-specific inhibition that will undoubtedly provide an invaluable tool for the further design of novel, potent, and specific therapeutics against the JAK family.

Reviews - 2b7a mentioned but not cited (6)

  1. The molecular regulation of Janus kinase (JAK) activation. Babon JJ, Lucet IS, Murphy JM, Nicola NA, Varghese LN. Biochem J 462 1-13 (2014)
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  6. Anticancer Activity of Natural and Synthetic Chalcones. Constantinescu T, Lungu CN. Int J Mol Sci 22 11306 (2021)

Articles - 2b7a mentioned but not cited (34)

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  15. Discovering RNA-protein interactome by using chemical context profiling of the RNA-protein interface. Parisien M, Wang X, Perdrizet G, Lamphear C, Fierke CA, Maheshwari KC, Wilde MJ, Sosnick TR, Pan T. Cell Rep 3 1703-1713 (2013)
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  20. Identified the Synergistic Mechanism of Drynariae Rhizoma for Treating Fracture Based on Network Pharmacology. Lin H, Wang X, Wang L, Dong H, Huang P, Cai Q, Mo Y, Huang F, Jiang Z. Evid Based Complement Alternat Med 2019 7342635 (2019)
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  23. Identification of tyrosine 972 as a novel site of Jak2 tyrosine kinase phosphorylation and its role in Jak2 activation. McDoom I, Ma X, Kirabo A, Lee KY, Ostrov DA, Sayeski PP. Biochemistry 47 8326-8334 (2008)
  24. Ab initio modeling and experimental assessment of Janus Kinase 2 (JAK2) kinase-pseudokinase complex structure. Wan X, Ma Y, McClendon CL, Huang LJ, Huang N. PLoS Comput Biol 9 e1003022 (2013)
  25. Nonlinear molecular dynamics of quercetin in Gynocardia odorata and Diospyros malabarica fruits: Its mechanistic role in hepatoprotection. Ghosh A, Sarmah P, Patel H, Mukerjee N, Mishra R, Alkahtani S, Varma RS, Baishya D. PLoS One 17 e0263917 (2022)
  26. Selaginellin B induces apoptosis and autophagy in pancreatic cancer cells via the JAK2/STAT3 signaling pathway. Chu P, Wang S, Zhu X, Yang Y, Li H, Tesfaldet T, Shopit A, Yang Y, Ma X, Peng J, Tang Z, Sun Z. Am J Transl Res 12 7127-7143 (2020)
  27. Computational analyses of JAK1 kinase domain: subtle changes in the catalytic cleft influence inhibitor specificity. Zhang X, Hu Y, Yuan Z. Biochem Biophys Res Commun 370 72-76 (2008)
  28. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Kim BH, Yi EH, Jee JG, Jeong AJ, Sandoval C, Park IC, Baeg GH, Ye SK. J Cell Mol Med 24 7427-7438 (2020)
  29. Lotus Bee Pollen Extract Inhibits Isoproterenol-Induced Hypertrophy via JAK2/STAT3 Signaling Pathway in Rat H9c2 Cells. Han S, Chen L, Zhang Y, Xie S, Yang J, Su S, Yao H, Shi P. Antioxidants (Basel) 12 88 (2022)
  30. A Comprehensive Evaluation of Sdox, a Promising H2S-Releasing Doxorubicin for the Treatment of Chemoresistant Tumors. Alov P, Al Sharif M, Aluani D, Chegaev K, Dinic J, Divac Rankov A, Fernandes MX, Fusi F, García-Sosa AT, Juvonen R, Kondeva-Burdina M, Padrón JM, Pajeva I, Pencheva T, Puerta A, Raunio H, Riganti C, Tsakovska I, Tzankova V, Yordanov Y, Saponara S. Front Pharmacol 13 831791 (2022)
  31. Comprehensive Bioinformatics Analysis Combined with Wet-Lab Experiments to Find Target Proteins of Chinese Medicine Monomer. Xu X, Zhu Y, Yue C, Yang Q, Zhang Z. Molecules 27 6105 (2022)
  32. Comprehensive analysis of crystal structure, spectroscopic properties, quantum chemical insights, and molecular docking studies of two pyrazolopyridine compounds: potential anticancer agents. Polo-Cuadrado E, López-Cuellar L, Acosta-Quiroga K, Rojas-Peña C, Brito I, Cisterna J, Trilleras J, Alderete JB, Duarte Y, Gutiérrez M. RSC Adv 13 30118-30128 (2023)
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  34. Network Pharmacology and Experimental Validation of the Anti-Inflammatory Effect of Tingli Dazao Xiefei Decoction in Acute Lung Injury Treatment. Zhang C, Li X, Gao D, Zhu H, Wang S, Tan B, Yang A. J Inflamm Res 16 6195-6209 (2023)


Reviews citing this publication (47)

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Articles citing this publication (87)

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  16. Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). Jiang JK, Ghoreschi K, Deflorian F, Chen Z, Perreira M, Pesu M, Smith J, Nguyen DT, Liu EH, Leister W, Costanzi S, O'Shea JJ, Thomas CJ. J Med Chem 51 8012-8018 (2008)
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