Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity.
Huang Y, Liu W, Zhao C, Shi X, Zhao Q, Jia J, Wang A.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2024.116547 PUBLICATION REGISTRY
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25 hitsDiscovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.
Xu Z, Liu Y, Song B, Ren B, Xu X, Lin R, Zhu X, Chen C, Yang S, Zhu Y, Jiang W, Li W, Xia Y, Hu L, Chen S, Chan CC, Li J, Zhang X, Yang L, Tian X, Ding CZ.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2024.129769Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents: <i>in silico</i> studies, synthesis, and biological evaluation.
Ghobish SA, Mohamed KO, Farag N, Farag DB.
RSC Med Chem · research-article; journal article · DOI 10.1039/d3md00524kFrom Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.
Shi Z, Tian L, Qiang T, Li J, Xing Y, Ren X, Liu C, Liang C.
J Med Chem · research support, non-u.s. gov't; systematic review; journal article · DOI 10.1021/acs.jmedchem.1c02064Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Liao M, Zhang J, Wang G, Wang L, Liu J, Ouyang L, Liu B.
J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.0c01180Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.
Lin T, Li J, Liu L, Li Y, Jiang H, Chen K, Xu P, Luo C, Zhou B.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113281FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
Wang S, Yuan XH, Wang SQ, Zhao W, Chen XB, Yu B.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.113218Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells.
Shi X, Quan Y, Wang Y, Wang Y, Li Y.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2020.127725Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?
Rassias G, Leonardi S, Rigopoulou D, Vachlioti E, Afratis K, Piperigkou Z, Koutsakis C, Karamanos NK, Gavras H, Papaioannou D.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112948First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.
Wei M, Zhao R, Cao Y, Wei Y, Li M, Dong Z, Liu Y, Ruan H, Li Y, Cao S, Tang Z, Zhou Y, Song W, Wang Y, Wang J, Yang G, Yang C.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112903Are all cyclin-dependent kinases 4/6 inhibitors created equal?
Marra A, Curigliano G.
NPJ Breast Cancer · review-article; review; journal article · DOI 10.1038/s41523-019-0121-yNovel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.
Wang X, Yu C, Wang C, Ma Y, Wang T, Li Y, Huang Z, Zhou M, Sun P, Zheng J, Yang S, Fan Y, Xiang R.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.07.038Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP.
Bioorg Med Chem Lett · research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2019.06.021Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.
Poratti M, Marzaro G.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.03.064Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.
Cheng W, Yang Z, Wang S, Li Y, Wei H, Tian X, Kan Q.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.01.003How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?
Jorda R, Hendrychová D, Voller J, Řezníčková E, Gucký T, Kryštof V.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b00049Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.
Li Y, Luo X, Guo Q, Nie Y, Wang T, Zhang C, Huang Z, Wang X, Liu Y, Chen Y, Zheng J, Yang S, Fan Y, Xiang R.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b00209Novel vitexin-inspired scaffold against leukemia.
Ling T, Lang W, Feng X, Das S, Maier J, Jeffries C, Shelat A, Rivas F.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.01.004A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.12.003The target landscape of clinical kinase drugs.
Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C, Zecha J, Reiter K, Qiao H, Helm D, Koch H, Schoof M, Canevari G, Casale E, Depaolini SR, Feuchtinger A, Wu Z, Schmidt T, Rueckert L, Becker W, Huenges J, Garz AK, Gohlke BO, Zolg DP, Kayser G, Vooder T, Preissner R, Hahne H, Tõnisson N, Kramer K, Götze K, Bassermann F, Schlegl J, Ehrlich HC, Aiche S, Walch A, Greif PA, Schneider S, Felder ER, Ruland J, Médard G, Jeremias I, Spiekermann K, Kuster B.
Science · research support, non-u.s. gov't; research-article; journal article · DOI 10.1126/science.aan4368Competitive Kinase Enrichment Proteomics Reveals that Abemaciclib Inhibits GSK3β and Activates WNT Signaling.
Cousins EM, Goldfarb D, Yan F, Roques J, Darr D, Johnson GL, Major MB.
Mol Cancer Res · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1158/1541-7786.mcr-17-0468Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.
Kalra S, Joshi G, Munshi A, Kumar R.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2017.08.071Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.
Li Y, Guo Q, Zhang C, Huang Z, Wang T, Wang X, Wang X, Xu G, Liu Y, Yang S, Fan Y, Xiang R.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.06.041Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.
Sánchez-Martínez C, Gelbert LM, Lallena MJ, de Dios A.
Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2015.05.100CDKN2A/p16 Loss Implicates CDK4 as a Therapeutic Target in Imatinib-Resistant Dermatofibrosarcoma Protuberans.
Eilers G, Czaplinski JT, Mayeda M, Bahri N, Tao D, Zhu M, Hornick JL, Lindeman NI, Sicinska E, Wagner AJ, Fletcher JA, Mariño-Enriquez A.
Mol Cancer Ther · research-article; journal article; research support, n.i.h., extramural · DOI 10.1158/1535-7163.mct-14-0793