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Structure-Activity Relationships and Discovery of (S)-5-(tert-Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido[2',1':2,3]imidazo[4,5-h]quinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer.
Gotchev D, Chen S, Dugan B, Dorsey BD, Wang X, Sheraz M, Kowalski R, Liu F, Tang S, Chiu T, Harasym T, Graves IE, Thi EP, Mason JD, Overholt N, Dugyala R, Lam AM, Cole AG, Sofia MJ. Gotchev D, et al. Among authors: cole ag. J Med Chem. 2024 Nov 28;67(22):20467-20494. doi: 10.1021/acs.jmedchem.4c01928. Epub 2024 Nov 8. J Med Chem. 2024. PMID: 39513566
Preclinical Profile of AB-423, an Inhibitor of Hepatitis B Virus Pregenomic RNA Encapsidation.
Mani N, Cole AG, Phelps JR, Ardzinski A, Cobarrubias KD, Cuconati A, Dorsey BD, Evangelista E, Fan K, Guo F, Guo H, Guo JT, Harasym TO, Kadhim S, Kultgen SG, Lee ACH, Li AHL, Long Q, Majeski SA, Mao R, McClintock KD, Reid SP, Rijnbrand R, Snead NM, Micolochick Steuer HM, Stever K, Tang S, Wang X, Zhao Q, Sofia MJ. Mani N, et al. Among authors: cole ag. Antimicrob Agents Chemother. 2018 May 25;62(6):e00082-18. doi: 10.1128/AAC.00082-18. Print 2018 Jun. Antimicrob Agents Chemother. 2018. PMID: 29555628 Free PMC article.
Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1.
Park JJ, Thi EP, Carpio VH, Bi Y, Cole AG, Dorsey BD, Fan K, Harasym T, Iott CL, Kadhim S, Kim JH, Lee ACH, Nguyen D, Paratala BS, Qiu R, White A, Lakshminarasimhan D, Leo C, Suto RK, Rijnbrand R, Tang S, Sofia MJ, Moore CB. Park JJ, et al. Among authors: cole ag. Nat Commun. 2021 Feb 22;12(1):1222. doi: 10.1038/s41467-021-21410-1. Nat Commun. 2021. PMID: 33619272 Free PMC article.
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: cole ag. 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.
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: cole ag. Antiviral Res. 2022 Jan;197:105211. doi: 10.1016/j.antiviral.2021.105211. Epub 2021 Nov 23. Antiviral Res. 2022. PMID: 34826506
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. 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.
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. 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: cole ag. 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: cole ag. 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: cole ag. 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
123 results