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A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.
Hills ID, Holloway MK, de León P, Nomland A, Zhu H, Rajapakse H, Allison TJ, Munshi SK, Colussi D, Pietrak BL, Toolan D, Haugabook SJ, Graham SL, Stachel SJ. Hills ID, et al. Among authors: de leon p. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4993-5. doi: 10.1016/j.bmcl.2009.07.071. Epub 2009 Jul 17. Bioorg Med Chem Lett. 2009. PMID: 19640712
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.
Rudd MT, Manley PJ, Hanney B, Meng Z, Shu Y, de Leon P, Frie JL, Han Y, Wai JM, Yang ZQ, Perkins JJ, Hurzy DM, Manikowski JJ, Zhu H, Bungard CJ, Converso A, Meissner RS, Cosden ML, Hayashi I, Ma L, O'Brien J, Uebele VN, Schachter JB, Bhandari N, Ward GJ, Fillgrove KL, Lu B, Liang Y, Dubost DC, Puri V, Eddins DM, Vardigan JD, Drolet RE, Kern JT, Uslaner JM. Rudd MT, et al. Among authors: de leon p. ACS Med Chem Lett. 2023 Jul 12;14(8):1088-1094. doi: 10.1021/acsmedchemlett.3c00210. eCollection 2023 Aug 10. ACS Med Chem Lett. 2023. PMID: 37583812 Free PMC article.
Optimization of 8-Hydroxyquinolines as Inhibitors of Catechol O-Methyltransferase.
Buchler I, Akuma D, Au V, Carr G, de León P, DePasquale M, Ernst G, Huang Y, Kimos M, Kolobova A, Poslusney M, Wei H, Swinnen D, Montel F, Moureau F, Jigorel E, Schulze MED, Wood M, Barrow JC. Buchler I, et al. Among authors: de leon p. J Med Chem. 2018 Nov 8;61(21):9647-9665. doi: 10.1021/acs.jmedchem.8b01126. Epub 2018 Oct 19. J Med Chem. 2018. PMID: 30272964 Free PMC article.
Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol O-Methyltransferase.
Ernst G, Akuma D, Au V, Buchler IP, Byers S, Carr GV, Defays S, de León P, Demaude T, DePasquale M, Durieu V, Huang Y, Jigorel E, Kimos M, Kolobova A, Montel F, Moureau F, Poslusney M, Swinnen D, Vandergeten MC, Van Houtvin N, Wei H, White N, Wood M, Barrow JC. Ernst G, et al. Among authors: de leon p. ACS Med Chem Lett. 2019 Oct 22;10(11):1573-1578. doi: 10.1021/acsmedchemlett.9b00345. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 32038769 Free PMC article.
Grandiose narcissism, unfounded beliefs, and behavioral reactions during the COVID-19 pandemic.
Żemojtel-Piotrowska M, Sawicki A, Piotrowski J, Lifshin U, Kretchner M, Skowronski JJ, Sedikides C, Jonason PK, Adamovic M, Ahmed O, Atitsogbe KA, Al-Shawaf L, Appiah SCY, Ardi R, Azam U, Babakr ZH, Baldursson EB, Bălțătescu S, Bochaver K, Bolatov A, Bonato M, Bundhoo HY, Chaleeraktrakoon T, Chobthamkit P, Cowden RG, Counted V, de Clunie G, Dragova-Koleva S, Esteves CS, Gouveia VV, Gundolf K, Hamouda S, Haretche C, Jeong EHK, Iliško D, Malik NI, Aruta JJB, Jia F, Jovanović V, Jukić T, Jukić DP, Kamble SV, Khachatryan N, Klicperova-Baker M, Kogler C, Knezović E, Koralov M, Kovacs M, Eldesoki WLM, Fernandez AL, Liik K, Malik S, Maltby J, Malysheva K, Mamuti A, Mangafic J, Moon C, Milfont TL, Muehlbacher S, Najafi R, Özsoy E, Park J, de León PP, Solcova IP, Ramos-Diaz J, Ridic G, Riđić O, Samekin A, Spoto A, Starc A, Stefenel D, Trà KTT, Tiliouine H, Tomšik R, Torres-Marín J, Umeh CS, Wills-Herrera E, Wlodarczyk A, Vally Z, Vauclair CM, Yahiiaiev I, Zand S. Żemojtel-Piotrowska M, et al. Among authors: de leon pp. Sci Rep. 2024 Jul 30;14(1):17503. doi: 10.1038/s41598-024-67954-2. Sci Rep. 2024. PMID: 39080302 Free PMC article.
134 results