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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
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
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 Apr 23. doi: 10.1021/acsinfecdis.4c00122. Online ahead of print. ACS Infect Dis. 2024. PMID: 38651692
Safety, pharmacokinetics, and antiviral activity of the capsid inhibitor AB-506 from Phase 1 studies in healthy subjects and those with hepatitis B.
Yuen MF, Berliba E, Sukeepaisarnjaroen W, Ahn SH, Tanwandee T, Lim YS, Kim YJ, Poovorawan K, Tangkijvanich P, Schwabe C, Eley T, Brown J, Lee ACH, Thi EP, Paratala B, Mani N, Sofia MJ, Picchio G, Sims KD, Gane EJ. Yuen MF, et al. Among authors: sofia mj. Hepatol Commun. 2022 Dec;6(12):3457-3472. doi: 10.1002/hep4.2095. Epub 2022 Oct 4. Hepatol Commun. 2022. PMID: 36194181 Free PMC article. Clinical Trial.
The identification of highly efficacious functionalised tetrahydrocyclopenta[c]pyrroles as inhibitors of HBV viral replication through modulation of HBV capsid assembly.
Cole AG, Kultgen SG, Mani N, Ardzinski A, Fan KY, Thi EP, Dorsey BD, Stever K, Chiu T, Tang S, Daly O, Phelps JR, Harasym T, Olland A, Suto RK, Sofia MJ. Cole AG, et al. Among authors: sofia mj. RSC Med Chem. 2022 Jan 19;13(3):343-349. doi: 10.1039/d1md00318f. eCollection 2022 Mar 23. RSC Med Chem. 2022. PMID: 35434625 Free PMC article.
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein.
Mani N, Cole AG, Phelps JR, Ardzinski A, Burns R, Chiu T, Cuconati A, Dorsey BD, Evangelista E, Fan K, Guo F, Harasym TO, Kadhim S, Kowalski R, Kultgen SG, Lee ACH, Li AH, Majeski SA, Miller A, Pasetka C, Reid SP, Rijnbrand R, Micolochick Steuer HM, Stever K, Tang S, Teng X, Wang X, Sofia MJ. Mani N, et al. Among authors: sofia mj. Antiviral Res. 2022 Jan;197:105211. doi: 10.1016/j.antiviral.2021.105211. Epub 2021 Nov 23. Antiviral Res. 2022. PMID: 34826506
Host Poly(A) Polymerases PAPD5 and PAPD7 Provide Two Layers of Protection That Ensure the Integrity and Stability of Hepatitis B Virus RNA.
Liu F, Lee ACH, Guo F, Kondratowicz AS, Micolochick Steuer HM, Miller A, Bailey LD, Wang X, Chen S, Kultgen SG, Cuconati A, Cole AG, Gotchev D, Dorsey BD, Rijnbrand R, Lam AM, Sofia MJ, Gao M. Liu F, et al. Among authors: sofia mj. J Virol. 2021 Aug 25;95(18):e0057421. doi: 10.1128/JVI.00574-21. Epub 2021 Aug 25. J Virol. 2021. PMID: 34191584 Free PMC article.
86 results