Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies.
Zhou Y, Kang J, Lu X.
J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.4c00361 PUBLIKATIONSREGISTRET
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Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115953Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Wang Z, Wang J, Wang Y, Xiang S, Zhou H, Song S, Song X, Tu Z, Zhou Y, Ding K, Zhang ZM, Zhang Z, Lu X.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c00899Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review.
El-Nassan HB, Al-Qadhi MA.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2023.115618Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.
Qin Q, Fu Q, Wang X, Lv R, Lu S, Guo Z, Wu T, Sun Y, Sun Y, Liu N, Zhao D, Cheng M.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115291Targeting Gatekeeper Mutations for Kinase Drug Discovery.
Zhou Y, Xiang S, Yang F, Lu X.
J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.2c01361Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.
Xiang S, Wang J, Huang H, Wang Z, Song X, Zhou Y, Jin F, He X, Zhang ZM, Tu Z, Ding K, Zhang Z, Lu X.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114899Discovery of 3-pyrazolyl-substituted pyrazolo[1,5-a]pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance.
Gong Y, Wu FX, Wang MS, Xu HC, Zhuo LS, Yang GF, Huang W.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114654Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.
Wu T, Qin Q, Lv R, Liu N, Yin W, Hao C, Sun Y, Zhang C, Sun Y, Zhao D, Cheng M.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114451Conformational adjustment overcomes multiple drug-resistance mutants of tropomyosin receptor kinase.
Mei LC, Zhuo LS, Xu HC, Huang W, Hao GF, Yang GF.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114406Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Wang Z, Wang J, Wang Y, Xiang S, Song X, Tu Z, Zhou Y, Zhang ZM, Zhang Z, Ding K, Lu X.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.2c00308Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6<i>H</i>-pyrimido[5,4-<i>b</i>][1,4]oxazin-7(8<i>H</i>)-one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant Mutants.
Pan S, Zhang L, Luo X, Nan J, Yang W, Bin H, Li Y, Huang Q, Wang T, Pan Z, Mu B, Wang F, Tian C, Liu Y, Li L, Yang S.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01597Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation.
Zhuo LS, Wang MS, Wu FX, Xu HC, Gong Y, Yu ZC, Tian YG, Pang C, Hao GF, Huang W, Yang GF.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01539Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.
Liu Z, Yu P, Dong L, Wang W, Duan S, Wang B, Gong X, Ye L, Wang H, Tian J.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c00712Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.
Li MC, Lin WH, Wang PC, Su YC, Chen PY, Fan CM, Chen CP, Huang CL, Chiu CH, Chang L, Chen CT, Yeh TK, Hsieh HP.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113673Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors.
Sun M, Cai S, Li P, Zhang F, Zhang H, Zhou J.
Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2020.115811Targeting tropomyosin receptor kinase for cancer therapy.
Miao Q, Ma K, Chen D, Wu X, Jiang S.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.04.053Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.
Yan W, Lakkaniga NR, Carlomagno F, Santoro M, McDonald NQ, Lv F, Gunaganti N, Frett B, Li HY.
J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.8b01092A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.
Drilon A, Nagasubramanian R, Blake JF, Ku N, Tuch BB, Ebata K, Smith S, Lauriault V, Kolakowski GR, Brandhuber BJ, Larsen PD, Bouhana KS, Winski SL, Hamor R, Wu WI, Parker A, Morales TH, Sullivan FX, DeWolf WE, Wollenberg LA, Gordon PR, Douglas-Lindsay DN, Scaltriti M, Benayed R, Raj S, Hanusch B, Schram AM, Jonsson P, Berger MF, Hechtman JF, Taylor BS, Andrews S, Rothenberg SM, Hyman DM.
Cancer Discov · clinical trial; research-article; journal article · DOI 10.1158/2159-8290.cd-17-0507