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Page 1
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease.
Candito DA, Simov V, Gulati A, Kattar S, Chau RW, Lapointe BT, Methot JL, DeMong DE, Graham TH, Kurukulasuriya R, Keylor MH, Tong L, Morriello GJ, Acton JJ, Pio B, Liu W, Scott JD, Ardolino MJ, Martinot TA, Maddess ML, Yan X, Gunaydin H, Palte RL, McMinn SE, Nogle L, Yu H, Minnihan EC, Lesburg CA, Liu P, Su J, Hegde LG, Moy LY, Woodhouse JD, Faltus R, Xiong T, Ciaccio P, Piesvaux JA, Otte KM, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Neelamkavil S, Wood HB, Fuller PH, Ellis JM. Candito DA, et al. Among authors: fuller ph. J Med Chem. 2022 Dec 22;65(24):16801-16817. doi: 10.1021/acs.jmedchem.2c01605. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475697
Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease.
Kattar SD, Gulati A, Margrey KA, Keylor MH, Ardolino M, Yan X, Johnson R, Palte RL, McMinn SE, Nogle L, Su J, Xiao D, Piesvaux J, Lee S, Hegde LG, Woodhouse JD, Faltus R, Moy LY, Xiong T, Ciaccio PJ, Pearson K, Patel M, Otte KM, Leyns CEG, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Fuller PH. Kattar SD, et al. Among authors: fuller ph. J Med Chem. 2023 Nov 9;66(21):14912-14927. doi: 10.1021/acs.jmedchem.3c01486. Epub 2023 Oct 20. J Med Chem. 2023. PMID: 37861679
Effects of LRRK2 Inhibitors in Nonhuman Primates.
Miller GK, Kuruvilla S, Jacob B, LaFranco-Scheuch L, Bakthavatchalu V, Flor J, Flor K, Ziegler J, Reichard C, Manfre P, Firner S, McNutt T, Quay D, Bellum S, Doto G, Ciaccio PJ, Pearson K, Valentine J, Fuller P, Fell M, Tsuchiya T, Williamson T, Wollenberg G. Miller GK, et al. Toxicol Pathol. 2023 Jul;51(5):232-245. doi: 10.1177/01926233231205895. Epub 2023 Nov 2. Toxicol Pathol. 2023. PMID: 37916535
Discovery and Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors.
Logan KM, Kaplan W, Simov V, Zhou H, Li D, Torres L, Morriello GJ, Acton JJ, Pio B, Chen YH, Keylor MH, Johnson R, Kattar SD, Chau R, Yan X, Ardolino M, Zarate C, Otte KM, Palte RL, Xiong T, McMinn SE, Lin S, Neelamkavil SF, Liu P, Su J, Hegde LG, Woodhouse JD, Moy LY, Ciaccio PJ, Piesvaux J, Zebisch M, Henry C, Barker J, Wood HB, Kennedy ME, DiMauro EF, Fell MJ, Fuller PH. Logan KM, et al. Among authors: fuller ph. J Med Chem. 2024 Sep 26;67(18):16807-16819. doi: 10.1021/acs.jmedchem.4c01627. Epub 2024 Sep 4. J Med Chem. 2024. PMID: 39231262
Total Synthesis of Aflastatin A.
Evans DA, Beiger JJ, Burch JD, Fuller PH, Glorius F, Kattnig E, Thaisrivongs DA, Trenkle WC, Young JM, Zhang J. Evans DA, et al. Among authors: fuller ph. J Am Chem Soc. 2022 Nov 2;144(43):19953-19972. doi: 10.1021/jacs.2c08244. Epub 2022 Oct 21. J Am Chem Soc. 2022. PMID: 36269121
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
Keylor MH, Gulati A, Kattar SD, Johnson RE, Chau RW, Margrey KA, Ardolino MJ, Zarate C, Poremba KE, Simov V, Morriello GJ, Acton JJ, Pio B, Yan X, Palte RL, McMinn SE, Nogle L, Lesburg CA, Adpressa D, Lin S, Neelamkavil S, Liu P, Su J, Hegde LG, Woodhouse JD, Faltus R, Xiong T, Ciaccio PJ, Piesvaux J, Otte KM, Wood HB, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Fuller PH. Keylor MH, et al. Among authors: fuller ph. J Med Chem. 2022 Jan 13;65(1):838-856. doi: 10.1021/acs.jmedchem.1c01968. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967623
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Gulati A, Yeung CS, Lapointe B, Kattar SD, Gunaydin H, Scott JD, Childers KK, Methot JL, Simov V, Kurukulasuriya R, Pio B, Morriello GJ, Liu P, Tang H, Neelamkavil S, Wood HB, Rada VL, Ardolino MJ, Yan XC, Palte R, Otte K, Faltus R, Woodhouse J, Hegde LG, Ciaccio P, Minnihan EC, DiMauro EF, Fell MJ, Fuller PH, Ellis JM. Gulati A, et al. Among authors: fuller ph. RSC Med Chem. 2021 Jun 4;12(7):1164-1173. doi: 10.1039/d1md00097g. eCollection 2021 Jul 21. RSC Med Chem. 2021. PMID: 34355182 Free PMC article.
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