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Page 1
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Perreault S, Chandrasekhar J, Cui ZH, Evarts J, Hao J, Kaplan JA, Kashishian A, Keegan KS, Kenney T, Koditek D, Lad L, Lepist EI, McGrath ME, Patel L, Phillips B, Therrien J, Treiberg J, Yahiaoui A, Phillips G. Perreault S, et al. Among authors: lad l. J Med Chem. 2017 Feb 23;60(4):1555-1567. doi: 10.1021/acs.jmedchem.6b01821. Epub 2017 Feb 7. J Med Chem. 2017. PMID: 28106991
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.
Patel L, Chandrasekhar J, Evarts J, Haran AC, Ip C, Kaplan JA, Kim M, Koditek D, Lad L, Lepist EI, McGrath ME, Novikov N, Perreault S, Puri KD, Somoza JR, Steiner BH, Stevens KL, Therrien J, Treiberg J, Villaseñor AG, Yeung A, Phillips G. Patel L, et al. Among authors: lad l. J Med Chem. 2016 Apr 14;59(7):3532-48. doi: 10.1021/acs.jmedchem.6b00213. Epub 2016 Mar 29. J Med Chem. 2016. PMID: 26980109
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.
Patel L, Chandrasekhar J, Evarts J, Forseth K, Haran AC, Ip C, Kashishian A, Kim M, Koditek D, Koppenol S, Lad L, Lepist EI, McGrath ME, Perreault S, Puri KD, Villaseñor AG, Somoza JR, Steiner BH, Therrien J, Treiberg J, Phillips G. Patel L, et al. Among authors: lad l. J Med Chem. 2016 Oct 13;59(19):9228-9242. doi: 10.1021/acs.jmedchem.6b01169. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27660855
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Among authors: lad l. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
Clinical targeting of HIV capsid protein with a long-acting small molecule.
Link JO, Rhee MS, Tse WC, Zheng J, Somoza JR, Rowe W, Begley R, Chiu A, Mulato A, Hansen D, Singer E, Tsai LK, Bam RA, Chou CH, Canales E, Brizgys G, Zhang JR, Li J, Graupe M, Morganelli P, Liu Q, Wu Q, Halcomb RL, Saito RD, Schroeder SD, Lazerwith SE, Bondy S, Jin D, Hung M, Novikov N, Liu X, Villaseñor AG, Cannizzaro CE, Hu EY, Anderson RL, Appleby TC, Lu B, Mwangi J, Liclican A, Niedziela-Majka A, Papalia GA, Wong MH, Leavitt SA, Xu Y, Koditek D, Stepan GJ, Yu H, Pagratis N, Clancy S, Ahmadyar S, Cai TZ, Sellers S, Wolckenhauer SA, Ling J, Callebaut C, Margot N, Ram RR, Liu YP, Hyland R, Sinclair GI, Ruane PJ, Crofoot GE, McDonald CK, Brainard DM, Lad L, Swaminathan S, Sundquist WI, Sakowicz R, Chester AE, Lee WE, Daar ES, Yant SR, Cihlar T. Link JO, et al. Among authors: lad l. Nature. 2020 Aug;584(7822):614-618. doi: 10.1038/s41586-020-2443-1. Epub 2020 Jul 1. Nature. 2020. PMID: 32612233 Free PMC article. Clinical Trial.
Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.
Qian X, McDonald A, Zhou HJ, Adams ND, Parrish CA, Duffy KJ, Fitch DM, Tedesco R, Ashcraft LW, Yao B, Jiang H, Huang JK, Marin MV, Aroyan CE, Wang J, Ahmed S, Burgess JL, Chaudhari AM, Donatelli CA, Darcy MG, Ridgers LH, Newlander KA, Schmidt SJ, Chai D, Colón M, Zimmerman MN, Lad L, Sakowicz R, Schauer S, Belmont L, Baliga R, Pierce DW, Finer JT, Wang Z, Morgan BP, Morgans DJ Jr, Auger KR, Sung CM, Carson JD, Luo L, Hugger ED, Copeland RA, Sutton D, Elliott JD, Jackson JR, Wood KW, Dhanak D, Bergnes G, Knight SD. Qian X, et al. Among authors: lad l. ACS Med Chem Lett. 2010 Jan 19;1(1):30-4. doi: 10.1021/ml900018m. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900171 Free PMC article.
Lipid-sensing high-throughput ApoA-I assays.
Niedziela-Majka A, Lad L, Chisholm JW, Lagpacan L, Schwartz K, Hung M, Jin D, Fung W, Brendza KM, Liu X, Pagratis N, Sakowicz R. Niedziela-Majka A, et al. Among authors: lad l. J Biomol Screen. 2012 Sep;17(8):1050-61. doi: 10.1177/1087057112451923. Epub 2012 Jul 17. J Biomol Screen. 2012. PMID: 22811478
34 results