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Molecular & Cellular Oncology Volume 9, 2022 - Issue 1
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Resistance to kinase inhibition through shortened target engagement

Aziz M. Rangwalaa Department of Pharmacological Sciences, Stony Brook University Renaissance School of Medicine, Stony Brook, NY, USACorrespondence[email protected]
ORCID Iconhttps://orcid.org/0000-0003-3556-7931View further author information
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Benedict-Tilman Bergerb Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt am Main, Germany;c Structural Genomics Consortium, Buchmann Institute for Life Sciences, Goethe University Frankfurt, Frankfurt am Main, GermanyORCID Iconhttps://orcid.org/0000-0002-3314-2617View further author information
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Matthew B. Robersd Research and Development Department, Promega Corporation, Fitchburg, WI, USAORCID Iconhttps://orcid.org/0000-0001-8505-5227View further author information
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Stefan Knappb Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt am Main, Germany;c Structural Genomics Consortium, Buchmann Institute for Life Sciences, Goethe University Frankfurt, Frankfurt am Main, GermanyORCID Iconhttps://orcid.org/0000-0001-5995-6494View further author information
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Markus A. Seeligera Department of Pharmacological Sciences, Stony Brook University Renaissance School of Medicine, Stony Brook, NY, USACorrespondence[email protected]
ORCID Iconhttps://orcid.org/0000-0003-0990-1756View further author information
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Article: 2029999 | Received 14 Dec 2021, Accepted 07 Jan 2022, Published online: 22 Jan 2022

References

  • Huse M, Kuriyan J. The conformational plasticity of protein kinases. Cell. 2002;109(3):275–3. doi:10.1016/S0092-8674(02)00741-9.
  • Foda ZH, Shan Y, Kim ET, Shaw DE, Seeliger MA. A dynamically coupled allosteric network underlies binding cooperativity in Src kinase. Nat Commun. 2015;6(1):5939. doi:10.1038/ncomms6939.
  • Shan Y, Kim ET, Eastwood MP, Dror RO, Seeliger MA, Shaw DE. How does a drug molecule find its target binding site? J Am Chem Soc. 2011;133(24):9181–9183. doi:10.1021/ja202726y.
  • Shekhar M, Smith Z, Seeliger M, Tiwary P. Protein flexibility and dissociation pathways differentiation can explain onset of resistance mutations: Abl kinase and Gleevec case study. BioRxiv. 2021. doi:10.1101/2021.07.02.450932.
  • Lu H, Tonge PJ. Drug–target residence time: critical information for lead optimization. Curr Opin Chem Biol. 2010;14(4):467–474. doi:10.1016/j.cbpa.2010.06.176.
  • Pargellis C, Tong L, Churchill L, Cirillo PF, Gilmore T, Graham AG, Grob PM, Hickey ER, Moss N, Pav S, Regan J. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat Struct Biol. 2002;9(4):268–272. doi:10.1038/nsb770.
  • Georgi V, Schiele F, Berger BT, Steffen A, Marin Zapata PA, Briem H, Menz S, Preusse C, Vasta JD, Robers MB, et al. Binding kinetics survey of the drugged kinome. J Am Chem Soc. 2018;140(46):15774–15782. doi:10.1021/jacs.8b08048.
  • Berger BT, Amaral M, Kokh DB, Nunes-Alves A, Musil D, Heinrich T, Schröder M, Neil R, Wang J, Navratilova I, et al. Structure-Kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2. Cell Chem Biol. 2021;28(5):686–698.e7. doi:10.1016/j.chembiol.2021.01.003.
  • Lyczek A, Berger BT, Rangwala AM, Paung Y, Tom J, Philipose H, Guo J, Albanese SK, Robers MB, Knapp S, et al. Mutation in Abl kinase with altered drug-binding kinetics indicates a novel mechanism of imatinib resistance. Proc Natl Acad Sci USA. 2021;118(46):e2111451118. doi:10.1073/pnas.2111451118.
  • Robers MB, Friedman-Ohana R, Huber KV, Kilpatrick L, Vasta JD, Berger BT, Chaudhry C, Hill S, Müller S, Knapp S, et al. Quantifying target occupancy of small molecules within living cells. Annu Rev Biochem. 2020;89(1):557–581. doi:10.1146/annurev-biochem-011420-092302.

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