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Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.
Heald RA, Jackson P, Savy P, Jones M, Gancia E, Burton B, Newman R, Boggs J, Chan E, Chan J, Choo E, Merchant M, Rudewicz P, Ultsch M, Wiesmann C, Yue Q, Belvin M, Price S. Heald RA, et al. Among authors: rudewicz p. J Med Chem. 2012 May 24;55(10):4594-604. doi: 10.1021/jm2017094. Epub 2012 May 3. J Med Chem. 2012. PMID: 22506516
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Barsanti PA, Pan Y, Lu Y, Jain R, Cox M, Aversa RJ, Dillon MP, Elling R, Hu C, Jin X, Knapp M, Lan J, Ramurthy S, Rudewicz P, Setti L, Subramanian S, Mathur M, Taricani L, Thomas G, Xiao L, Yue Q. Barsanti PA, et al. Among authors: rudewicz p. ACS Med Chem Lett. 2014 Oct 30;6(1):42-6. doi: 10.1021/ml500352s. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589928 Free PMC article.
Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
Nagle A, Biggart A, Be C, Srinivas H, Hein A, Caridha D, Sciotti RJ, Pybus B, Kreishman-Deitrick M, Bursulaya B, Lai YH, Gao MY, Liang F, Mathison CJN, Liu X, Yeh V, Smith J, Lerario I, Xie Y, Chianelli D, Gibney M, Berman A, Chen YL, Jiricek J, Davis LC, Liu X, Ballard J, Khare S, Eggimann FK, Luneau A, Groessl T, Shapiro M, Richmond W, Johnson K, Rudewicz PJ, Rao SPS, Thompson C, Tuntland T, Spraggon G, Glynne RJ, Supek F, Wiesmann C, Molteni V. Nagle A, et al. Among authors: rudewicz pj. J Med Chem. 2020 Oct 8;63(19):10773-10781. doi: 10.1021/acs.jmedchem.0c00499. Epub 2020 Jul 29. J Med Chem. 2020. PMID: 32667203 Free PMC article.
Discovery of Potent and Selective Antibody-Drug Conjugates with Eg5 Inhibitors through Linker and Payload Optimization.
Karpov AS, Nieto-Oberhuber CM, Abrams T, Beng-Louka E, Blanco E, Chamoin S, Chene P, Dacquignies I, Daniel D, Dillon MP, Doumampouom-Metoul L, Drosos N, Fedoseev P, Furegati M, Granda B, Grotzfeld RM, Hess Clark S, Joly E, Jones D, Lacaud-Baumlin M, Lagasse-Guerro S, Lorenzana EG, Mallet W, Martyniuk P, Marzinzik AL, Mesrouze Y, Nocito S, Oei Y, Perruccio F, Piizzi G, Richard E, Rudewicz PJ, Schindler P, Velay M, Venstrom K, Wang P, Zurini M, Lafrance M. Karpov AS, et al. Among authors: rudewicz pj. ACS Med Chem Lett. 2019 Dec 3;10(12):1674-1679. doi: 10.1021/acsmedchemlett.9b00468. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857845 Free PMC article.
Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae - Identification of LYS228.
Reck F, Bermingham A, Blais J, Capka V, Cariaga T, Casarez A, Colvin R, Dean CR, Fekete A, Gong W, Growcott E, Guo H, Jones AK, Li C, Li F, Lin X, Lindvall M, Lopez S, McKenney D, Metzger L, Moser HE, Prathapam R, Rasper D, Rudewicz P, Sethuraman V, Shen X, Shaul J, Simmons RL, Tashiro K, Tang D, Tjandra M, Turner N, Uehara T, Vitt C, Whitebread S, Yifru A, Zang X, Zhu Q. Reck F, et al. Among authors: rudewicz p. Bioorg Med Chem Lett. 2018 Feb 15;28(4):748-755. doi: 10.1016/j.bmcl.2018.01.006. Epub 2018 Jan 4. Bioorg Med Chem Lett. 2018. PMID: 29336873
36 results