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Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering.
Gu C, Lamb ML, Johannes JW, Sylvester MA, Eisman MS, Harrison RA, Hu H, Kazmirski S, Mikule K, Peng B, Su N, Wang W, Ye Q, Zheng X, Lyne PD, Scott DA. Gu C, et al. Among authors: wang w. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4775-4780. doi: 10.1016/j.bmcl.2016.08.030. Epub 2016 Aug 12. Bioorg Med Chem Lett. 2016. PMID: 27578247
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Johannes JW, Almeida L, Daly K, Ferguson AD, Grosskurth SE, Guan H, Howard T, Ioannidis S, Kazmirski S, Lamb ML, Larsen NA, Lyne PD, Mikule K, Ogoe C, Peng B, Petteruti P, Read JA, Su N, Sylvester M, Throner S, Wang W, Wang X, Wu J, Ye Q, Yu Y, Zheng X, Scott DA. Johannes JW, et al. Among authors: wang x, wang w. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5743-7. doi: 10.1016/j.bmcl.2015.10.079. Epub 2015 Oct 27. Bioorg Med Chem Lett. 2015. PMID: 26546219
Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer.
Wang Z, Grosskurth SE, Cheung T, Petteruti P, Zhang J, Wang X, Wang W, Gharahdaghi F, Wu J, Su N, Howard RT, Mayo M, Widzowski D, Scott DA, Johannes JW, Lamb ML, Lawson D, Dry JR, Lyne PD, Tate EW, Zinda M, Mikule K, Fawell SE, Reimer C, Chen H. Wang Z, et al. Among authors: wang x, wang w. Cancer Res. 2018 Dec 1;78(23):6691-6702. doi: 10.1158/0008-5472.CAN-18-1362. Epub 2018 Oct 8. Cancer Res. 2018. PMID: 30297535 Free article.
AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.
Rhyasen GW, Hattersley MM, Yao Y, Dulak A, Wang W, Petteruti P, Dale IL, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh TC, Rabow AA, Dry JR, Reimer C, Lyne P, Mills GB, Fawell SE, Waring MJ, Zinda M, Clark E, Chen H. Rhyasen GW, et al. Among authors: wang w. Mol Cancer Ther. 2016 Nov;15(11):2563-2574. doi: 10.1158/1535-7163.MCT-16-0141. Epub 2016 Aug 29. Mol Cancer Ther. 2016. PMID: 27573426
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q. Katz JD, et al. Among authors: wang w. J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24. J Med Chem. 2011. PMID: 21608528
Potent and selective bivalent inhibitors of BET bromodomains.
Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale I, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Méndez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y. Waring MJ, et al. Among authors: wang w. Nat Chem Biol. 2016 Dec;12(12):1097-1104. doi: 10.1038/nchembio.2210. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775716
Efficacious intermittent dosing of a novel JAK2 inhibitor in mouse models of polycythemia vera.
Kraus M, Wang Y, Aleksandrowicz D, Bachman E, Szewczak AA, Walker D, Xu L, Bouthillette M, Childers KM, Dolinski B, Haidle AM, Kopinja J, Lee L, Lim J, Little KD, Ma Y, Mathur A, Mo JR, O'Hare E, Otte RD, Taoka BM, Wang W, Yin H, Zabierek AA, Zhang W, Zhao S, Zhu J, Young JR, Marshall CG. Kraus M, et al. Among authors: wang w, wang y. PLoS One. 2012;7(5):e37207. doi: 10.1371/journal.pone.0037207. Epub 2012 May 18. PLoS One. 2012. PMID: 22623993 Free PMC article.
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