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Discovery of Novel UDP-N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa.
Ryan MD, Parkes AL, Corbett D, Dickie AP, Southey M, Andersen OA, Stein DB, Barbeau OR, Sanzone A, Thommes P, Barker J, Cain R, Compper C, Dejob M, Dorali A, Etheridge D, Evans S, Faulkner A, Gadouleau E, Gorman T, Haase D, Holbrow-Wilshaw M, Krulle T, Li X, Lumley C, Mertins B, Napier S, Odedra R, Papadopoulos K, Roumpelakis V, Spear K, Trimby E, Williams J, Zahn M, Keefe AD, Zhang Y, Soutter HT, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Deng B, Hunt A, Sigel EA, Troast DM, DeJonge BLM. Ryan MD, et al. J Med Chem. 2021 Oct 14;64(19):14377-14425. doi: 10.1021/acs.jmedchem.1c00888. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34569791
Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB.
Mesleh MF, Cross JB, Zhang J, Kahmann J, Andersen OA, Barker J, Cheng RK, Felicetti B, Wood M, Hadfield AT, Scheich C, Moy TI, Yang Q, Shotwell J, Nguyen K, Lippa B, Dolle R, Ryan MD. Mesleh MF, et al. Among authors: ryan md. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1314-8. doi: 10.1016/j.bmcl.2016.01.009. Epub 2016 Jan 6. Bioorg Med Chem Lett. 2016. PMID: 26786695
Structure-based discovery of LpxC inhibitors.
Zhang J, Chan A, Lippa B, Cross JB, Liu C, Yin N, Romero JA, Lawrence J, Heney R, Herradura P, Goss J, Clark C, Abel C, Zhang Y, Poutsiaka KM, Epie F, Conrad M, Mahamoon A, Nguyen K, Chavan A, Clark E, Li TC, Cheng RK, Wood M, Andersen OA, Brooks M, Kwong J, Barker J, Parr IB, Gu Y, Ryan MD, Coleman S, Metcalf CA 3rd. Zhang J, et al. Among authors: ryan md. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1670-1680. doi: 10.1016/j.bmcl.2017.03.006. Epub 2017 Mar 6. Bioorg Med Chem Lett. 2017. PMID: 28302397
Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.
Cross JB, Zhang J, Yang Q, Mesleh MF, Romero JA, Wang B, Bevan D, Poutsiaka KM, Epie F, Moy T, Daniel A, Shotwell J, Chamberlain B, Carter N, Andersen O, Barker J, Ryan MD, Metcalf CA 3rd, Silverman J, Nguyen K, Lippa B, Dolle RE. Cross JB, et al. Among authors: ryan md. ACS Med Chem Lett. 2016 Feb 16;7(4):374-8. doi: 10.1021/acsmedchemlett.5b00368. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096044 Free PMC article.
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Kallander LS, Lu Q, Chen W, Tomaszek T, Yang G, Tew D, Meek TD, Hofmann GA, Schulz-Pritchard CK, Smith WW, Janson CA, Ryan MD, Zhang GF, Johanson KO, Kirkpatrick RB, Ho TF, Fisher PW, Mattern MR, Johnson RK, Hansbury MJ, Winkler JD, Ward KW, Veber DF, Thompson SK. Kallander LS, et al. Among authors: ryan md. J Med Chem. 2005 Sep 8;48(18):5644-7. doi: 10.1021/jm050408c. J Med Chem. 2005. PMID: 16134930
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
Marino JP Jr, Fisher PW, Hofmann GA, Kirkpatrick RB, Janson CA, Johnson RK, Ma C, Mattern M, Meek TD, Ryan MD, Schulz C, Smith WW, Tew DG, Tomazek TA Jr, Veber DF, Xiong WC, Yamamoto Y, Yamashita K, Yang G, Thompson SK. Marino JP Jr, et al. Among authors: ryan md. J Med Chem. 2007 Aug 9;50(16):3777-85. doi: 10.1021/jm061182w. Epub 2007 Jul 18. J Med Chem. 2007. PMID: 17636946
Potent and selective nonpeptide inhibitors of caspases 3 and 7.
Lee D, Long SA, Murray JH, Adams JL, Nuttall ME, Nadeau DP, Kikly K, Winkler JD, Sung CM, Ryan MD, Levy MA, Keller PM, DeWolf WE Jr. Lee D, et al. Among authors: ryan md. J Med Chem. 2001 Jun 7;44(12):2015-26. doi: 10.1021/jm0100537. J Med Chem. 2001. PMID: 11384246
In-silico guided discovery of novel CCR9 antagonists.
Zhang X, Cross JB, Romero J, Heifetz A, Humphries E, Hall K, Wu Y, Stucka S, Zhang J, Chandonnet H, Lippa B, Ryan MD, Baber JC. Zhang X, et al. Among authors: ryan md. J Comput Aided Mol Des. 2018 Apr;32(4):573-582. doi: 10.1007/s10822-018-0113-2. Epub 2018 Mar 26. J Comput Aided Mol Des. 2018. PMID: 29582229
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
Christensen SB, Guider A, Forster CJ, Gleason JG, Bender PE, Karpinski JM, DeWolf WE Jr, Barnette MS, Underwood DC, Griswold DE, Cieslinski LB, Burman M, Bochnowicz S, Osborn RR, Manning CD, Grous M, Hillegas LM, Bartus JO, Ryan MD, Eggleston DS, Haltiwanger RC, Torphy TJ. Christensen SB, et al. Among authors: ryan md. J Med Chem. 1998 Mar 12;41(6):821-35. doi: 10.1021/jm970090r. J Med Chem. 1998. PMID: 9526558
Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality.
Lee D, Long SA, Adams JL, Chan G, Vaidya KS, Francis TA, Kikly K, Winkler JD, Sung CM, Debouck C, Richardson S, Levy MA, DeWolf WE Jr, Keller PM, Tomaszek T, Head MS, Ryan MD, Haltiwanger RC, Liang PH, Janson CA, McDevitt PJ, Johanson K, Concha NO, Chan W, Abdel-Meguid SS, Badger AM, Lark MW, Nadeau DP, Suva LJ, Gowen M, Nuttall ME. Lee D, et al. Among authors: ryan md. J Biol Chem. 2000 May 26;275(21):16007-14. doi: 10.1074/jbc.275.21.16007. J Biol Chem. 2000. PMID: 10821855 Free article.
181 results