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Page 1
Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV-2 Mpro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition against Pan-Coronavirus Homologues and Nirmatrelvir-Resistant Variants.
Wang X, Gotchev D, Fan KY, Vega MM, Mani N, McGovern-Gooch K, Cuconati A, Tercero B, Wang X, Carpino P, Maskos K, Centrella PA, Schmitt A, Preuss F, Prasad A, Chen CY, Clark MA, Guilinger JP, Johnstone S, von König K, Keefe AD, Liu J, Turcotte S, Zhang Y, Konz Makino DL, Lam AM, Cole AG, Sofia MJ. Wang X, et al. Among authors: sofia mj. J Med Chem. 2024 Nov 14;67(21):19623-19667. doi: 10.1021/acs.jmedchem.4c02009. Epub 2024 Oct 25. J Med Chem. 2024. PMID: 39453309
Design, synthesis, and structure-activity relationship of a bicyclic HBV capsid assembly modulator chemotype leading to the identification of clinical candidate AB-506.
Cole AG, Kultgen SG, Mani N, Quintero JG, Yi Fan K, Ardzinski A, Stever K, Dorsey BD, Phelps JR, Lee ACH, Thi EP, Chiu T, Tang S, Horanyi PS, Mayclin SJ, Harasym TO, Sofia MJ. Cole AG, et al. Among authors: sofia mj. Bioorg Med Chem Lett. 2023 Oct 1;94:129456. doi: 10.1016/j.bmcl.2023.129456. Epub 2023 Aug 25. Bioorg Med Chem Lett. 2023. PMID: 37633618
Structure-Activity Relationships and Discovery of (S)-6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro-6H-pyrido[1,2-h][1,7]naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer.
Gotchev D, Dorsey BD, Nguyen D, Kakarla R, Dugan B, Chen S, Gao M, Bailey L, Liu F, Harasym T, Chiu T, Tang S, Lee AC, Cole AG, Sofia MJ. Gotchev D, et al. Among authors: sofia mj. J Med Chem. 2024 Jan 25;67(2):1421-1446. doi: 10.1021/acs.jmedchem.3c01981. Epub 2024 Jan 8. J Med Chem. 2024. PMID: 38190324
Preclinical Antiviral and Safety Profiling of the HBV RNA Destabilizer AB-161.
Lam AM, Dugyala RR, Sheraz M, Liu F, Thi EP, Graves IE, Cuconati A, Steuer HM, Ardzinski A, Overholt N, Mason JD, Gotchev D, Cole AG, Harasym TO, Sofia MJ. Lam AM, et al. Among authors: sofia mj. Viruses. 2024 Feb 21;16(3):323. doi: 10.3390/v16030323. Viruses. 2024. PMID: 38543689 Free PMC article.
Discovery of C-Linked Nucleoside Analogues with Antiviral Activity against SARS-CoV-2.
Mesaros EF, Dugan BJ, Gao M, Sheraz M, McGovern-Gooch K, Xu F, Fan KY, Nguyen D, Kultgen SG, Lindstrom A, Stever K, Tercero B, Binder RJ, Liu F, Micolochick Steuer HM, Mani N, Harasym TO, Thi EP, Cuconati A, Dorsey BD, Cole AG, Lam AM, Sofia MJ. Mesaros EF, et al. Among authors: sofia mj. ACS Infect Dis. 2024 May 10;10(5):1780-1792. doi: 10.1021/acsinfecdis.4c00122. Epub 2024 Apr 23. ACS Infect Dis. 2024. PMID: 38651692
Rational Design, Synthesis, and Structure-Activity Relationship of a Novel Isoquinolinone-Based Series of HBV Capsid Assembly Modulators Leading to the Identification of Clinical Candidate AB-836.
Cole AG, Kultgen SG, Mani N, Fan KY, Ardzinski A, Stever K, Dorsey BD, Mesaros EF, Thi EP, Graves I, Tang S, Harasym TO, Lee ACH, Olland A, Suto RK, Sofia MJ. Cole AG, et al. Among authors: sofia mj. J Med Chem. 2024 Sep 26;67(18):16773-16795. doi: 10.1021/acs.jmedchem.4c01568. Epub 2024 Sep 4. J Med Chem. 2024. PMID: 39231272
Conformationally Constrained Isoquinolinones as Orally Efficacious Hepatitis B Capsid Assembly Modulators.
Mesaros EF, Cole AG, Kultgen SG, Mani N, Fan KY, Dugan BJ, Ardzinski A, Stever K, Micolochick Steuer HM, Graves I, Tang S, Harasym TO, Lam AM, Thi EP, Dorsey BD, Sofia MJ. Mesaros EF, et al. Among authors: sofia mj. ACS Med Chem Lett. 2024 Sep 3;15(9):1627-1634. doi: 10.1021/acsmedchemlett.4c00388. eCollection 2024 Sep 12. ACS Med Chem Lett. 2024. PMID: 39291037
Control of Hepatitis B Virus with Imdusiran, a Small Interfering RNA Therapeutic.
Thi EP, Ye X, Snead NM, Lee ACH, Micolochick Steuer HM, Ardzinski A, Graves IE, Espiritu C, Cuconati A, Abbott C, Jarosz A, Teng X, Paratala B, McClintock K, Harasym T, Rijnbrand R, Lam AM, Sofia MJ. Thi EP, et al. Among authors: sofia mj. ACS Infect Dis. 2024 Oct 11;10(10):3640-3649. doi: 10.1021/acsinfecdis.4c00514. Epub 2024 Sep 22. ACS Infect Dis. 2024. PMID: 39306863
Preclinical and clinical antiviral characterization of AB-836, a potent capsid assembly modulator against hepatitis B virus.
Lam AM, Mani N, Ardzinski A, Stever K, Cuconati A, Micolochick Steuer H, Thi EP, Graves IE, Espiritu CL, Mesaros E, Kultgen SG, Fan K, Cole AG, Harasym TO, Rijnbrand R, Brown J, Eley T, Varughese T, Gane E, Picchio G, Sims KD, Sofia MJ. Lam AM, et al. Among authors: sofia mj. Antiviral Res. 2024 Nov;231:106010. doi: 10.1016/j.antiviral.2024.106010. Epub 2024 Sep 24. Antiviral Res. 2024. PMID: 39326502
93 results