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Page 1
Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.
Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS. Olson CM, et al. Among authors: leggett a. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10. doi: 10.1016/j.chembiol.2019.02.012. Epub 2019 Mar 21. Cell Chem Biol. 2019. PMID: 30905681 Free PMC article.
SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform.
Hatcher JM, Wu G, Zeng C, Zhu J, Meng F, Patel S, Wang W, Ficarro SB, Leggett AL, Powell CE, Marto JA, Zhang K, Ki Ngo JC, Fu XD, Zhang T, Gray NS. Hatcher JM, et al. Among authors: leggett al. Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6. doi: 10.1016/j.chembiol.2018.01.013. Epub 2018 Feb 22. Cell Chem Biol. 2018. PMID: 29478907 Free PMC article.
Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13.
Zeng M, Kwiatkowski NP, Zhang T, Nabet B, Xu M, Liang Y, Quan C, Wang J, Hao M, Palakurthi S, Zhou S, Zeng Q, Kirschmeier PT, Meghani K, Leggett AL, Qi J, Shapiro GI, Liu JF, Matulonis UA, Lin CY, Konstantinopoulos PA, Gray NS. Zeng M, et al. Among authors: leggett al. Elife. 2018 Nov 13;7:e39030. doi: 10.7554/eLife.39030. Elife. 2018. PMID: 30422115 Free PMC article.
Discovery of a selective inhibitor of doublecortin like kinase 1.
Ferguson FM, Nabet B, Raghavan S, Liu Y, Leggett AL, Kuljanin M, Kalekar RL, Yang A, He S, Wang J, Ng RWS, Sulahian R, Li L, Poulin EJ, Huang L, Koren J, Dieguez-Martinez N, Espinosa S, Zeng Z, Corona CR, Vasta JD, Ohi R, Sim T, Kim ND, Harshbarger W, Lizcano JM, Robers MB, Muthaswamy S, Lin CY, Look AT, Haigis KM, Mancias JD, Wolpin BM, Aguirre AJ, Hahn WC, Westover KD, Gray NS. Ferguson FM, et al. Among authors: leggett al. Nat Chem Biol. 2020 Jun;16(6):635-643. doi: 10.1038/s41589-020-0506-0. Epub 2020 Apr 6. Nat Chem Biol. 2020. PMID: 32251410 Free PMC article.
EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma.
Iniguez AB, Stolte B, Wang EJ, Conway AS, Alexe G, Dharia NV, Kwiatkowski N, Zhang T, Abraham BJ, Mora J, Kalev P, Leggett A, Chowdhury D, Benes CH, Young RA, Gray NS, Stegmaier K. Iniguez AB, et al. Among authors: leggett a. Cancer Cell. 2018 Feb 12;33(2):202-216.e6. doi: 10.1016/j.ccell.2017.12.009. Epub 2018 Jan 18. Cancer Cell. 2018. PMID: 29358035 Free PMC article.
CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer.
Zhang H, Christensen CL, Dries R, Oser MG, Deng J, Diskin B, Li F, Pan Y, Zhang X, Yin Y, Papadopoulos E, Pyon V, Thakurdin C, Kwiatkowski N, Jani K, Rabin AR, Castro DM, Chen T, Silver H, Huang Q, Bulatovic M, Dowling CM, Sundberg B, Leggett A, Ranieri M, Han H, Li S, Yang A, Labbe KE, Almonte C, Sviderskiy VO, Quinn M, Donaghue J, Wang ES, Zhang T, He Z, Velcheti V, Hammerman PS, Freeman GJ, Bonneau R, Kaelin WG Jr, Sutherland KD, Kersbergen A, Aguirre AJ, Yuan GC, Rothenberg E, Miller G, Gray NS, Wong KK. Zhang H, et al. Among authors: leggett a. Cancer Cell. 2020 Jan 13;37(1):37-54.e9. doi: 10.1016/j.ccell.2019.11.003. Epub 2019 Dec 26. Cancer Cell. 2020. PMID: 31883968 Free PMC article.
Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression.
Rusan M, Li K, Li Y, Christensen CL, Abraham BJ, Kwiatkowski N, Buczkowski KA, Bockorny B, Chen T, Li S, Rhee K, Zhang H, Chen W, Terai H, Tavares T, Leggett AL, Li T, Wang Y, Zhang T, Kim TJ, Hong SH, Poudel-Neupane N, Silkes M, Mudianto T, Tan L, Shimamura T, Meyerson M, Bass AJ, Watanabe H, Gray NS, Young RA, Wong KK, Hammerman PS. Rusan M, et al. Among authors: leggett al. Cancer Discov. 2018 Jan;8(1):59-73. doi: 10.1158/2159-8290.CD-17-0461. Epub 2017 Oct 20. Cancer Discov. 2018. PMID: 29054992 Free PMC article.
The dTAG system for immediate and target-specific protein degradation.
Nabet B, Roberts JM, Buckley DL, Paulk J, Dastjerdi S, Yang A, Leggett AL, Erb MA, Lawlor MA, Souza A, Scott TG, Vittori S, Perry JA, Qi J, Winter GE, Wong KK, Gray NS, Bradner JE. Nabet B, et al. Among authors: leggett al. Nat Chem Biol. 2018 May;14(5):431-441. doi: 10.1038/s41589-018-0021-8. Epub 2018 Mar 26. Nat Chem Biol. 2018. PMID: 29581585 Free PMC article.
Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules.
Nabet B, Ferguson FM, Seong BKA, Kuljanin M, Leggett AL, Mohardt ML, Robichaud A, Conway AS, Buckley DL, Mancias JD, Bradner JE, Stegmaier K, Gray NS. Nabet B, et al. Among authors: leggett al. Nat Commun. 2020 Sep 18;11(1):4687. doi: 10.1038/s41467-020-18377-w. Nat Commun. 2020. PMID: 32948771 Free PMC article.
128 results