5ut6 Citations

JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

ACS Med Chem Lett 8 614-617 (2017)
Related entries: 5ut4, 5ut5

Cited: 18 times
EuropePMC logo PMID: 28626520

Abstract

A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe molecules with the pseudokinase JAK2 JH2 allosteric site. The syntheses of the fluorescent

Reviews - 5ut6 mentioned but not cited (1)

  1. Prospects for pharmacological targeting of pseudokinases. Kung JE, Jura N. Nat Rev Drug Discov 18 501-526 (2019)

Articles - 5ut6 mentioned but not cited (5)

  1. Convolutional neural network scoring and minimization in the D3R 2017 community challenge. Sunseri J, King JE, Francoeur PG, Koes DR, Koes DR. J Comput Aided Mol Des 33 19-34 (2019)
  2. JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules. Newton AS, Deiana L, Puleo DE, Cisneros JA, Cutrona KJ, Schlessinger J, Jorgensen WL. ACS Med Chem Lett 8 614-617 (2017)
  3. Discovery and evaluation of ZT55, a novel highly-selective tyrosine kinase inhibitor of JAK2V617F against myeloproliferative neoplasms. Hu M, Xu C, Yang C, Zuo H, Chen C, Zhang D, Shi G, Wang W, Shi J, Zhang T. J Exp Clin Cancer Res 38 49 (2019)
  4. eTOX ALLIES: an automated pipeLine for linear interaction energy-based simulations. Capoferri L, van Dijk M, Rustenburg AS, Wassenaar TA, Kooi DP, Rifai EA, Vermeulen NPE, Geerke DP. J Cheminform 9 58 (2017)
  5. Network pharmacology and RNA sequencing studies on triterpenoid saponins from Bupleurum chinense for the treatment of breast cancer. Li D, Liu D, Yue D, Gao P, Du C, Liu X, Zhang L. RSC Adv 9 41088-41098 (2019)


Reviews citing this publication (1)

  1. A Comprehensive Overview of Globally Approved JAK Inhibitors. Shawky AM, Almalki FA, Abdalla AN, Abdelazeem AH, Gouda AM. Pharmaceutics 14 1001 (2022)

Articles citing this publication (11)

  1. Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells. Foulkes DM, Byrne DP, Yeung W, Shrestha S, Bailey FP, Ferries S, Eyers CE, Keeshan K, Wells C, Drewry DH, Zuercher WJ, Kannan N, Eyers PA. Sci Signal 11 eaat7951 (2018)
  2. Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core. Liosi ME, Krimmer SG, Newton AS, Dawson TK, Puleo DE, Cutrona KJ, Suzuki Y, Schlessinger J, Jorgensen WL. J Med Chem 63 5324-5340 (2020)
  3. Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands. Liosi ME, Ippolito JA, Henry SP, Krimmer SG, Newton AS, Cutrona KJ, Olivarez RA, Mohanty J, Schlessinger J, Jorgensen WL. J Med Chem 65 8380-8400 (2022)
  4. Metadynamics as a Postprocessing Method for Virtual Screening with Application to the Pseudokinase Domain of JAK2. Cutrona KJ, Newton AS, Krimmer SG, Tirado-Rives J, Jorgensen WL. J Chem Inf Model 60 4403-4415 (2020)
  5. Hyperactivation of Oncogenic JAK3 Mutants Depend on ATP Binding to the Pseudokinase Domain. Raivola J, Hammarén HM, Virtanen AT, Bulleeraz V, Ward AC, Silvennoinen O. Front Oncol 8 560 (2018)
  6. Indoloxytriazines as binding molecules for the JAK2 JH2 pseudokinase domain and its V617F variant. Newton AS, Liosi ME, Henry SP, Deiana L, Faver JC, Krimmer SG, Puleo DE, Schlessinger J, Jorgensen WL. Tetrahedron Lett 77 153248 (2021)
  7. Conversion of a False Virtual Screen Hit into Selective JAK2 JH2 Domain Binders Using Convergent Design Strategies. Henry SP, Liosi ME, Ippolito JA, Cutrona KJ, Krimmer SG, Newton AS, Schlessinger J, Jorgensen WL. ACS Med Chem Lett 13 819-826 (2022)
  8. Covalent Modification of the JH2 Domain of Janus Kinase 2. Henry SP, Liosi ME, Ippolito JA, Menges F, Newton AS, Schlessinger J, Jorgensen WL. ACS Med Chem Lett 13 1819-1826 (2022)
  9. Diverse saturated heterocycles from a hydroacylation/conjugate addition cascade. Iwumene NUN, Moseley DF, Pullin RDC, Willis MC. Chem Sci 13 1504-1511 (2022)
  10. Identification of Novel Small Molecule Ligands for JAK2 Pseudokinase Domain. Virtanen AT, Haikarainen T, Sampathkumar P, Palmroth M, Liukkonen S, Liu J, Nekhotiaeva N, Hubbard SR, Silvennoinen O. Pharmaceuticals (Basel) 16 75 (2023)
  11. Role of water in the determination of protonation states of titratable residues. Zia SR. J Mol Model 27 61 (2021)