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Discovery of efficacious Pseudomonas aeruginosa-targeted siderophore-conjugated monocarbams by application of a semi-mechanistic pharmacokinetic/pharmacodynamic model.
Murphy-Benenato KE, Bhagunde PR, Chen A, Davis HE, Durand-Réville TF, Ehmann DE, Galullo V, Harris JJ, Hatoum-Mokdad H, Jahić H, Kim A, Manjunatha MR, Manyak EL, Mueller J, Patey S, Quiroga O, Rooney M, Sha L, Shapiro AB, Sylvester M, Tan B, Tsai AS, Uria-Nickelsen M, Wu Y, Zambrowski M, Zhao SX. Murphy-Benenato KE, et al. Among authors: chen a. J Med Chem. 2015 Mar 12;58(5):2195-205. doi: 10.1021/jm501506f. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25658376
Pharmacodynamic Profiling of a Siderophore-Conjugated Monocarbam in Pseudomonas aeruginosa: Assessing the Risk for Resistance and Attenuated Efficacy.
Kim A, Kutschke A, Ehmann DE, Patey SA, Crandon JL, Gorseth E, Miller AA, McLaughlin RE, Blinn CM, Chen A, Nayar AS, Dangel B, Tsai AS, Rooney MT, Murphy-Benenato KE, Eakin AE, Nicolau DP. Kim A, et al. Among authors: chen a. Antimicrob Agents Chemother. 2015 Dec;59(12):7743-52. doi: 10.1128/AAC.00831-15. Epub 2015 Oct 5. Antimicrob Agents Chemother. 2015. PMID: 26438502 Free PMC article.
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
Durand-Réville TF, Comita-Prevoir J, Zhang J, Wu X, May-Dracka TL, Romero JAC, Wu F, Chen A, Shapiro AB, Carter NM, McLeod SM, Giacobbe RA, Verheijen JC, Lahiri SD, Sacco MD, Chen Y, O'Donnell JP, Miller AA, Mueller JP, Tommasi RA. Durand-Réville TF, et al. Among authors: chen a, chen y. J Med Chem. 2020 Nov 12;63(21):12511-12525. doi: 10.1021/acs.jmedchem.0c00579. Epub 2020 Jul 24. J Med Chem. 2020. PMID: 32658473 Free PMC article.
N-Hydroxyformamide LpxC inhibitors, their in vivo efficacy in a mouse Escherichia coli infection model, and their safety in a rat hemodynamic assay.
Furuya T, Shapiro AB, Comita-Prevoir J, Kuenstner EJ, Zhang J, Ribe SD, Chen A, Hines D, Moussa SH, Carter NM, Sylvester MA, Romero JAC, Vega CV, Sacco MD, Chen Y, O'Donnell JP, Durand-Reville TF, Miller AA, Tommasi RA. Furuya T, et al. Among authors: chen a, chen y. Bioorg Med Chem. 2020 Dec 15;28(24):115826. doi: 10.1016/j.bmc.2020.115826. Epub 2020 Oct 28. Bioorg Med Chem. 2020. PMID: 33160146
Rational design of a new antibiotic class for drug-resistant infections.
Durand-Reville TF, Miller AA, O'Donnell JP, Wu X, Sylvester MA, Guler S, Iyer R, Shapiro AB, Carter NM, Velez-Vega C, Moussa SH, McLeod SM, Chen A, Tanudra AM, Zhang J, Comita-Prevoir J, Romero JA, Huynh H, Ferguson AD, Horanyi PS, Mayclin SJ, Heine HS, Drusano GL, Cummings JE, Slayden RA, Tommasi RA. Durand-Reville TF, et al. Among authors: chen a. Nature. 2021 Sep;597(7878):698-702. doi: 10.1038/s41586-021-03899-0. Epub 2021 Sep 15. Nature. 2021. PMID: 34526714
Pharmacokinetics of the natural antibiotic negamycin.
Guo J, Miele EW, Chen A, Luzietti RA, Zambrowski M, Walsky RL, Buurman ET. Guo J, et al. Among authors: chen a. Xenobiotica. 2015;45(7):625-33. doi: 10.3109/00498254.2015.1006301. Epub 2015 Mar 3. Xenobiotica. 2015. PMID: 25733027
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Bregman H, Berry L, Buchanan JL, Chen A, Du B, Feric E, Hierl M, Huang L, Immke D, Janosky B, Johnson D, Li X, Ligutti J, Liu D, Malmberg A, Matson D, McDermott J, Miu P, Nguyen HN, Patel VF, Waldon D, Wilenkin B, Zheng XM, Zou A, McDonough SI, DiMauro EF. Bregman H, et al. Among authors: chen a. J Med Chem. 2011 Jul 14;54(13):4427-45. doi: 10.1021/jm200018k. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634377
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, Lin J, Moriguchi J, Berry L, Huang L, Teffera Y, Yang Y, Zhang Y, Bellon SF, Lee M, Shimanovich R, Bak A, Dominguez C, Norman MH, Harmange JC, Dussault I, Kim TS. Liu L, et al. Among authors: chen a. J Med Chem. 2008 Jul 10;51(13):3688-91. doi: 10.1021/jm800401t. Epub 2008 Jun 14. J Med Chem. 2008. PMID: 18553959
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