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Linking High-Throughput Screens to Identify MoAs and Novel Inhibitors of Mycobacterium tuberculosis Dihydrofolate Reductase.
Santa Maria JP Jr, Park Y, Yang L, Murgolo N, Altman MD, Zuck P, Adam G, Chamberlin C, Saradjian P, Dandliker P, Boshoff HIM, Barry CE 3rd, Garlisi C, Olsen DB, Young K, Glick M, Nickbarg E, Kutchukian PS. Santa Maria JP Jr, et al. Among authors: garlisi c. ACS Chem Biol. 2017 Sep 15;12(9):2448-2456. doi: 10.1021/acschembio.7b00468. Epub 2017 Aug 29. ACS Chem Biol. 2017. PMID: 28806050 Free PMC article.
Kibdelomycin is a bactericidal broad-spectrum aerobic antibacterial agent.
Singh SB, Dayananth P, Balibar CJ, Garlisi CG, Lu J, Kishii R, Takei M, Fukuda Y, Ha S, Young K. Singh SB, et al. Antimicrob Agents Chemother. 2015;59(6):3474-81. doi: 10.1128/AAC.00382-15. Epub 2015 Apr 6. Antimicrob Agents Chemother. 2015. PMID: 25845866 Free PMC article.
Selective small-molecule inhibition of an RNA structural element.
Howe JA, Wang H, Fischmann TO, Balibar CJ, Xiao L, Galgoci AM, Malinverni JC, Mayhood T, Villafania A, Nahvi A, Murgolo N, Barbieri CM, Mann PA, Carr D, Xia E, Zuck P, Riley D, Painter RE, Walker SS, Sherborne B, de Jesus R, Pan W, Plotkin MA, Wu J, Rindgen D, Cummings J, Garlisi CG, Zhang R, Sheth PR, Gill CJ, Tang H, Roemer T. Howe JA, et al. Among authors: garlisi cg. Nature. 2015 Oct 29;526(7575):672-7. doi: 10.1038/nature15542. Epub 2015 Sep 30. Nature. 2015. PMID: 26416753
Chemical Genomics-Based Antifungal Drug Discovery: Targeting Glycosylphosphatidylinositol (GPI) Precursor Biosynthesis.
Mann PA, McLellan CA, Koseoglu S, Si Q, Kuzmin E, Flattery A, Harris G, Sher X, Murgolo N, Wang H, Devito K, de Pedro N, Genilloud O, Kahn JN, Jiang B, Costanzo M, Boone C, Garlisi CG, Lindquist S, Roemer T. Mann PA, et al. Among authors: garlisi cg. ACS Infect Dis. 2015 Jan 9;1(1):59-72. doi: 10.1021/id5000212. Epub 2014 Dec 12. ACS Infect Dis. 2015. PMID: 26878058 Free PMC article.
TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.
Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T. Lee SH, et al. Among authors: garlisi cg. Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364. Sci Transl Med. 2016. PMID: 26962156
In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.
Tan CM, Gill CJ, Wu J, Toussaint N, Yin J, Tsuchiya T, Garlisi CG, Kaelin D, Meinke PT, Miesel L, Olsen DB, Lagrutta A, Fukuda H, Kishii R, Takei M, Oohata K, Takeuchi T, Shibue T, Takano H, Nishimura A, Fukuda Y, Singh SB. Tan CM, et al. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4830-9. doi: 10.1128/AAC.00619-16. Print 2016 Aug. Antimicrob Agents Chemother. 2016. PMID: 27246784 Free PMC article.
Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase.
Walker SS, Labroli M, Painter RE, Wiltsie J, Sherborne B, Murgolo N, Sher X, Mann P, Zuck P, Garlisi CG, Su J, Kargman S, Xiao L, Scapin G, Salowe S, Devito K, Sheth P, Buist N, Tan CM, Black TA, Roemer T. Walker SS, et al. PLoS One. 2017 Jul 10;12(7):e0180965. doi: 10.1371/journal.pone.0180965. eCollection 2017. PLoS One. 2017. PMID: 28700746 Free PMC article.
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Mandal M, Xiao L, Pan W, Scapin G, Li G, Tang H, Yang SW, Pan J, Root Y, de Jesus RK, Yang C, Prosise W, Dayananth P, Mirza A, Therien AG, Young K, Flattery A, Garlisi C, Zhang R, Chu D, Sheth P, Chu I, Wu J, Markgraf C, Kim HY, Painter R, Mayhood TW, DiNunzio E, Wyss DF, Buevich AV, Fischmann T, Pasternak A, Dong S, Hicks JD, Villafania A, Liang L, Murgolo N, Black T, Hagmann WK, Tata J, Parmee ER, Weber AE, Su J, Tang H. Mandal M, et al. Among authors: garlisi c. J Med Chem. 2022 Dec 22;65(24):16234-16251. doi: 10.1021/acs.jmedchem.2c00766. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475645
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
Seganish WM, Fischmann TO, Sherborne B, Matasi J, Lavey B, McElroy WT, Tulshian D, Tata J, Sondey C, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. Seganish WM, et al. Among authors: garlisi cg. ACS Med Chem Lett. 2015 Jul 12;6(8):942-7. doi: 10.1021/acsmedchemlett.5b00279. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288698 Free PMC article.
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.
McElroy WT, Tan Z, Ho G, Paliwal S, Li G, Seganish WM, Tulshian D, Tata J, Fischmann TO, Sondey C, Bian H, Bober L, Jackson J, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. McElroy WT, et al. Among authors: garlisi cg. ACS Med Chem Lett. 2015 May 12;6(6):677-82. doi: 10.1021/acsmedchemlett.5b00106. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101573 Free PMC article.
62 results