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Page 1
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: hegde lg. 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
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: hegde lg. 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
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: hegde lg. 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: hegde lg. 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.
Characterization of the Onset, Progression, and Reversibility of Morphological Changes in Mouse Lung after Pharmacological Inhibition of Leucine-Rich Kinase 2 Kinase Activity.
Bryce DK, Ware CM, Woodhouse JD, Ciaccio PJ, Ellis JM, Hegde LG, Kuruvilla S, Maddess ML, Markgraf CG, Otte KM, Poulet FM, Timmins LM, Kennedy ME, Fell MJ. Bryce DK, et al. Among authors: hegde lg. J Pharmacol Exp Ther. 2021 Apr;377(1):11-19. doi: 10.1124/jpet.120.000217. Epub 2021 Jan 28. J Pharmacol Exp Ther. 2021. PMID: 33509901
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K. Zhang H, et al. Among authors: hegde lg. ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071676 Free PMC article.
Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI).
McKinnell RM, Fatheree P, Choi SK, Gendron R, Jendza K, Olson Blair B, Budman J, Hill CM, Hegde LG, Yu C, McConn D, Hegde SS, Marquess DG, Klein U. McKinnell RM, et al. Among authors: hegde lg. ACS Med Chem Lett. 2018 Dec 3;10(1):86-91. doi: 10.1021/acsmedchemlett.8b00462. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655952 Free PMC article.
Inhibition of RORγT Skews TCRα Gene Rearrangement and Limits T Cell Repertoire Diversity.
Guo Y, MacIsaac KD, Chen Y, Miller RJ, Jain R, Joyce-Shaikh B, Ferguson H, Wang IM, Cristescu R, Mudgett J, Engstrom L, Piers KJ, Baltus GA, Barr K, Zhang H, Mehmet H, Hegde LG, Hu X, Carter LL, Aicher TD, Glick G, Zaller D, Hawwari A, Correll CC, Jones DC, Cua DJ. Guo Y, et al. Among authors: hegde lg. Cell Rep. 2016 Dec 20;17(12):3206-3218. doi: 10.1016/j.celrep.2016.11.073. Cell Rep. 2016. PMID: 28009290 Free article.
Concomitant angiotensin AT1 receptor antagonism and neprilysin inhibition produces omapatrilat-like antihypertensive effects without promoting tracheal plasma extravasation in the rat.
Hegde LG, Yu C, Renner T, Thibodeaux H, Armstrong SR, Park T, Cheruvu M, Olsufka R, Sandvik ER, Lane CE, Budman J, Hill CM, Klein U, Hegde SS. Hegde LG, et al. J Cardiovasc Pharmacol. 2011 Apr;57(4):495-504. doi: 10.1097/FJC.0b013e318210fc7e. J Cardiovasc Pharmacol. 2011. PMID: 21297495
24 results