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From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack AM, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Among authors: parthasarathy g. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3. doi: 10.1016/j.chembiol.2019.10.002. Epub 2019 Oct 22. Cell Chem Biol. 2020. PMID: 31653597 Free article.
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack A, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Among authors: parthasarathy g. Cell Chem Biol. 2021 Feb 18;28(2):243. doi: 10.1016/j.chembiol.2021.01.019. Cell Chem Biol. 2021. PMID: 33607006 Free article. No abstract available.
The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.
Forster AB, Abeywickrema P, Bunda J, Cox CD, Cabalu TD, Egbertson M, Fay J, Getty K, Hall D, Kornienko M, Lu J, Parthasarathy G, Reid J, Sharma S, Shipe WD, Smith SM, Soisson S, Stachel SJ, Su HP, Wang D, Berger R. Forster AB, et al. Among authors: parthasarathy g. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5167-5171. doi: 10.1016/j.bmcl.2017.10.054. Epub 2017 Oct 23. Bioorg Med Chem Lett. 2017. PMID: 29113762
Identification of an allosteric binding site for RORγt inhibition.
Scheepstra M, Leysen S, van Almen GC, Miller JR, Piesvaux J, Kutilek V, van Eenennaam H, Zhang H, Barr K, Nagpal S, Soisson SM, Kornienko M, Wiley K, Elsen N, Sharma S, Correll CC, Trotter BW, van der Stelt M, Oubrie A, Ottmann C, Parthasarathy G, Brunsveld L. Scheepstra M, et al. Among authors: parthasarathy g. Nat Commun. 2015 Dec 7;6:8833. doi: 10.1038/ncomms9833. Nat Commun. 2015. PMID: 26640126 Free PMC article.
Restoring methicillin-resistant Staphylococcus aureus susceptibility to β-lactam antibiotics.
Tan CM, Therien AG, Lu J, Lee SH, Caron A, Gill CJ, Lebeau-Jacob C, Benton-Perdomo L, Monteiro JM, Pereira PM, Elsen NL, Wu J, Deschamps K, Petcu M, Wong S, Daigneault E, Kramer S, Liang L, Maxwell E, Claveau D, Vaillancourt J, Skorey K, Tam J, Wang H, Meredith TC, Sillaots S, Wang-Jarantow L, Ramtohul Y, Langlois E, Landry F, Reid JC, Parthasarathy G, Sharma S, Baryshnikova A, Lumb KJ, Pinho MG, Soisson SM, Roemer T. Tan CM, et al. Among authors: parthasarathy g. Sci Transl Med. 2012 Mar 21;4(126):126ra35. doi: 10.1126/scitranslmed.3003592. Sci Transl Med. 2012. PMID: 22440737
Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.
Stachel SJ, Egbertson MS, Wai J, Machacek M, Toolan DM, Swestock J, Eddins DM, Puri V, McGaughey G, Su HP, Perlow D, Wang D, Ma L, Parthasarathy G, Reid JC, Abeywickrema PD, Smith SM, Uslaner JM. Stachel SJ, et al. Among authors: parthasarathy g. Bioorg Med Chem Lett. 2018 Apr 1;28(6):1122-1126. doi: 10.1016/j.bmcl.2018.01.039. Epub 2018 Feb 10. Bioorg Med Chem Lett. 2018. PMID: 29534798
Identification of potent inhibitors of the sortilin-progranulin interaction.
Stachel SJ, Ginnetti AT, Johnson SA, Cramer P, Wang Y, Bukhtiyarova M, Krosky D, Stump C, Hurzy DM, Schlegel KA, Cooke AJ, Allen S, O'Donnell G, Ziebell M, Parthasarathy G, Getty KL, Ho T, Ou Y, Jovanovska A, Carroll SS, Pausch M, Lumb K, Mosser SD, Voleti B, Klein DJ, Soisson SM, Zerbinatti C, Coleman PJ. Stachel SJ, et al. Among authors: parthasarathy g. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127403. doi: 10.1016/j.bmcl.2020.127403. Epub 2020 Jul 15. Bioorg Med Chem Lett. 2020. PMID: 32738972
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: parthasarathy g. 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.
103 results