Discovery of KRB-456, a KRAS G12D Switch-I/II Allosteric Pocket Binder That Inhibits the Growth of Pancreatic Cancer Patient-derived Tumors.

Autor: Kazi A; Department of Pharmacology and Toxicology and Massey Comprehensive Cancer Center, Virginia Commonwealth University, Richmond, Virginia.; Drug Discovery Department, Moffitt Cancer Center, Tampa, Florida., Ranjan A; Department of Pharmacology and Toxicology and Massey Comprehensive Cancer Center, Virginia Commonwealth University, Richmond, Virginia., Kumar M V V; Department of Biochemistry, Department of Medicine, Montefiore Einstein Comprehensive Cancer Center, Albert Einstein College of Medicine, Bronx, New York., Agianian B; Department of Biochemistry, Department of Medicine, Montefiore Einstein Comprehensive Cancer Center, Albert Einstein College of Medicine, Bronx, New York., Garcia Chavez M; Department of Chemistry, Cancer Center at Illinois, University of Illinois at Urbana-Champaign, Urbana, Illinois., Vudatha V; Department of Surgery, Virginia Commonwealth University, Richmond, Virginia., Wang R; Department of Pharmacology and Toxicology and Massey Comprehensive Cancer Center, Virginia Commonwealth University, Richmond, Virginia., Vangipurapu R; Drug Discovery Department, Moffitt Cancer Center, Tampa, Florida., Chen L; Drug Discovery Department, Moffitt Cancer Center, Tampa, Florida., Kennedy P; Drug Discovery Department, Moffitt Cancer Center, Tampa, Florida., Subramanian K; Department of Pharmacology and Toxicology and Massey Comprehensive Cancer Center, Virginia Commonwealth University, Richmond, Virginia., Quirke JCK; Department of Chemistry, Cancer Center at Illinois, University of Illinois at Urbana-Champaign, Urbana, Illinois., Beato F; Department of Gastrointestinal Oncology, Moffitt Cancer Center, Tampa, Florida., Underwood PW; Department of Surgery, University of Florida, Gainesville, Florida., Fleming JB; Department of Gastrointestinal Oncology, Moffitt Cancer Center, Tampa, Florida., Trevino J; Department of Surgery, Virginia Commonwealth University, Richmond, Virginia.; Department of Surgery, University of Florida, Gainesville, Florida., Hergenrother PJ; Department of Chemistry, Cancer Center at Illinois, University of Illinois at Urbana-Champaign, Urbana, Illinois., Gavathiotis E; Department of Biochemistry, Department of Medicine, Montefiore Einstein Comprehensive Cancer Center, Albert Einstein College of Medicine, Bronx, New York., Sebti SM; Department of Pharmacology and Toxicology and Massey Comprehensive Cancer Center, Virginia Commonwealth University, Richmond, Virginia.; Drug Discovery Department, Moffitt Cancer Center, Tampa, Florida.

Publikováno v: Cancer research communications [Cancer Res Commun] 2023 Dec 28; Vol. 3 (12), pp. 2623-2639.

GH47 and Other Glycoside Hydrolases Catalyze Glycosidic Bond Cleavage with the Assistance of Substrate Super-arming at the Transition State.

Autor: Quirke JCK; Department of Pharmaceutical and Biomedical Sciences, University of Georgia, 250 West Green Street, Athens, GA 30602, USA.; Department of Chemistry, University of Georgia, 140 Cedar Street, Athens, GA 30602, USA.; Complex Carbohydrate Research Center, University of Georgia, 315 Riverbend Road, Athens, GA 30602, USA., Crich D; Department of Pharmaceutical and Biomedical Sciences, University of Georgia, 250 West Green Street, Athens, GA 30602, USA.; Department of Chemistry, University of Georgia, 140 Cedar Street, Athens, GA 30602, USA.; Complex Carbohydrate Research Center, University of Georgia, 315 Riverbend Road, Athens, GA 30602, USA.

Publikováno v: ACS catalysis [ACS Catal] 2021 Aug 20; Vol. 11, pp. 10308-10315. Date of Electronic Publication: 2021 Aug 04.

An Advanced Apralog with Increased in vitro and in vivo Activity toward Gram-negative Pathogens and Reduced ex vivo Cochleotoxicity.

Autor: Sonousi A; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI, 48202, USA., Quirke JCK; Department of Pharmacy and Biomedical Sciences and Department of Chemistry and Complex Carbohydrate Research Center, University of Georgia, 250 West Green Street, Athens, GA, 30602, USA., Waduge P; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI, 48202, USA., Janusic T; Institute of Medical Microbiology, University of Zurich, Gloriastrasse 28, 8006, Zürich, Switzerland., Gysin M; Institute of Medical Microbiology, University of Zurich, Gloriastrasse 28, 8006, Zürich, Switzerland., Haldimann K; Institute of Medical Microbiology, University of Zurich, Gloriastrasse 28, 8006, Zürich, Switzerland., Xu S; Department of Pathology and Laboratory Medicine, Medical University of South Carolina, Walton Research Building, Room 403-E, 39 Sabin Street, Charleston, SC, 29425, USA., Hobbie SN; Institute of Medical Microbiology, University of Zurich, Gloriastrasse 28, 8006, Zürich, Switzerland., Sha SH; Department of Pathology and Laboratory Medicine, Medical University of South Carolina, Walton Research Building, Room 403-E, 39 Sabin Street, Charleston, SC, 29425, USA., Schacht J; Kresge Hearing Research Institute, Department of Otolaryngology, University of Michigan, 1150 West Medical Center Drive, Ann Arbor, MI, 48109, USA., Chow CS; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI, 48202, USA., Vasella A; Organic Chemistry Laboratory, ETH Zürich, Vladimir-Prelog-Weg 1-5/10, 8093, Zürich, Switzerland., Böttger EC; Institute of Medical Microbiology, University of Zurich, Gloriastrasse 28, 8006, Zürich, Switzerland., Crich D; Department of Pharmacy and Biomedical Sciences and Department of Chemistry and Complex Carbohydrate Research Center, University of Georgia, 250 West Green Street, Athens, GA, 30602, USA.; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI, 48202, USA.

Publikováno v: ChemMedChem [ChemMedChem] 2021 Jan 19; Vol. 16 (2), pp. 335-339. Date of Electronic Publication: 2020 Oct 23.

Apralogs: Apramycin 5- O -Glycosides and Ethers with Improved Antibacterial Activity and Ribosomal Selectivity and Reduced Susceptibility to the Aminoacyltranserferase (3)-IV Resistance Determinant.

Autor: Quirke JCK; Department of Pharmaceutical and Biomedical Sciences , University of Georgia , 250 West Green Street , Athens , Georgia 30602 , United States.; Department of Chemistry , University of Georgia , 140 Cedar Street , Athens , Georgia 30602 , United States.; Complex Carbohydrate Research Center , University of Georgia , 315 Riverbend Road , Athens , Georgia 30602 , United States.; Department of Chemistry , Wayne State University , 5101 Cass Avenue , Detroit , Michigan 48202 , United States., Rajasekaran P; Department of Pharmaceutical and Biomedical Sciences , University of Georgia , 250 West Green Street , Athens , Georgia 30602 , United States.; Complex Carbohydrate Research Center , University of Georgia , 315 Riverbend Road , Athens , Georgia 30602 , United States.; Department of Chemistry , Wayne State University , 5101 Cass Avenue , Detroit , Michigan 48202 , United States., Sarpe VA; Department of Pharmaceutical and Biomedical Sciences , University of Georgia , 250 West Green Street , Athens , Georgia 30602 , United States.; Complex Carbohydrate Research Center , University of Georgia , 315 Riverbend Road , Athens , Georgia 30602 , United States.; Department of Chemistry , Wayne State University , 5101 Cass Avenue , Detroit , Michigan 48202 , United States., Sonousi A; Department of Chemistry , Wayne State University , 5101 Cass Avenue , Detroit , Michigan 48202 , United States., Osinnii I; Institute of Medical Microbiology , University of Zurich , Gloriastrasse 28 , 8006 Zürich , Switzerland., Gysin M; Institute of Medical Microbiology , University of Zurich , Gloriastrasse 28 , 8006 Zürich , Switzerland., Haldimann K; Institute of Medical Microbiology , University of Zurich , Gloriastrasse 28 , 8006 Zürich , Switzerland., Fang QJ; Department of Pathology and Laboratory Medicine , Medical University of South Carolina , Walton Research Building, Room 403-E, 39 Sabin Street , Charleston , South Carolina 29425 , United States., Shcherbakov D; Institute of Medical Microbiology , University of Zurich , Gloriastrasse 28 , 8006 Zürich , Switzerland., Hobbie SN; Institute of Medical Microbiology , University of Zurich , Gloriastrasse 28 , 8006 Zürich , Switzerland., Sha SH; Department of Pathology and Laboratory Medicine , Medical University of South Carolina , Walton Research Building, Room 403-E, 39 Sabin Street , Charleston , South Carolina 29425 , United States., Schacht J; Kresge Hearing Research Institute, Department of Otolaryngology , University of Michigan , 1150 West Medical Center Drive , Ann Arbor , Michigan 48109 , United States., Vasella A; Organic Chemistry Laboratory , ETH Zürich , Vladimir-Prelog-Weg 1-5/10 , 8093 Zürich , Switzerland., Böttger EC; Institute of Medical Microbiology , University of Zurich , Gloriastrasse 28 , 8006 Zürich , Switzerland., Crich D; Department of Pharmaceutical and Biomedical Sciences , University of Georgia , 250 West Green Street , Athens , Georgia 30602 , United States.; Department of Chemistry , University of Georgia , 140 Cedar Street , Athens , Georgia 30602 , United States.; Complex Carbohydrate Research Center , University of Georgia , 315 Riverbend Road , Athens , Georgia 30602 , United States.; Department of Chemistry , Wayne State University , 5101 Cass Avenue , Detroit , Michigan 48202 , United States.

Publikováno v: Journal of the American Chemical Society [J Am Chem Soc] 2020 Jan 08; Vol. 142 (1), pp. 530-544. Date of Electronic Publication: 2019 Dec 17.