Identification and Optimization of cell active 4-anilino-quin(az)oline Inhibitors for Protein Kinase Novel 3 (PKN3)

Autor: Asquith Crm, David H. Drewry, Carrow I. Wells, Sinha P, Kwarcinski Fe, Zutshi R, Tuomo Laitinen, Julie E. Pickett, Graham J. Tizzard, Louisa Temme

The development of a small library of 4-anilinoquinolines led to the identification of 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor of Protein Kinase Novel 3 (PKN3) with an IC50 of 1.3 μM in cells. Compound 16 presents

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f53ab4afff3c96be199df7ee7bbe88b3

Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

Autor: Asquith Crm, William J. Zuercher, Tammy M. Havener, David H. Drewry, David C Morris, Michael P. East, Carrow I. Wells, Kaleb M. Naegeli, Tuomo Laitinen, Gary L. Johnson

We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ea03975bfcb3d12bbb7c8886b8c4356

Pentathiepins are an understudied molecular prism of biological activities.

Autor: Pozzetti L; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio, Finland., Asquith CRM; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio, Finland.

Publikováno v: Archiv der Pharmazie [Arch Pharm (Weinheim)] 2024 Oct 09, pp. e2400646. Date of Electronic Publication: 2024 Oct 09.

PIP4K2C inhibition reverses autophagic flux impairment induced by SARS-CoV-2.

Autor: Karim M; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Mishra M; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Lo CW; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Saul S; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Cagirici HB; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Tran DHN; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Agrawal A; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Ghita L; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., Ojha A; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA., East MP; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Gammeltoft KA; Department of Infectious Diseases, University of Copenhagen, Denmark. Copenhagen Hepatitis C Program (CO-HEP), Department of Infectious Diseases, Copenhagen.; University Hospital-Hvidovre, Hvidovre, Denmark.; Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark., Sahoo MK; Department of Pathology, Stanford University School of Medicine, Stanford, California, USA., Johnson GL; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA., Das S; Biomedical & Nutritional Science, Center for Pathogen Research & Training (CPRT), University of Massachusetts-Lowell, USA., Jochmans D; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium., Cohen CA; US Army Medical Research Institute of Infectious Diseases, Viral Immunology Branch, Frederick, Maryland, USA., Gottwein J; Department of Infectious Diseases, University of Copenhagen, Denmark. Copenhagen Hepatitis C Program (CO-HEP), Department of Infectious Diseases, Copenhagen.; University Hospital-Hvidovre, Hvidovre, Denmark.; Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark., Dye J; US Army Medical Research Institute of Infectious Diseases, Viral Immunology Branch, Frederick, Maryland, USA., Neff N; Chan Zuckerberg Biohub, San Francisco, CA, 94158, USA., Pinsky BA; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA.; Department of Pathology, Stanford University School of Medicine, Stanford, California, USA., Laitinen T; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Finland., Pantsar T; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Finland., Poso A; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Finland., Zanini F; School of Clinical Medicine, UNSW Sydney, Sydney, New South Wales, Australia.; Cellular Genomics Futures Institute, UNSW Sydney, Sydney, New South Wales, Australia.; Evolution and Ecology Research Centre, UNSW Sydney, Sydney, New South Wales, Australia., Jonghe S; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium., Asquith CRM; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Finland., Einav S; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, California, USA.; Chan Zuckerberg Biohub, San Francisco, CA, 94158, USA.; Department of Microbiology and Immunology, Stanford University, CA, USA.

Publikováno v: BioRxiv : the preprint server for biology [bioRxiv] 2024 Apr 17. Date of Electronic Publication: 2024 Apr 17.

Discovery and Optimization of Narrow Spectrum Inhibitors of Tousled Like Kinase 2 (TLK2) Using Quantitative Structure Activity Relationships.

Autor: Asquith CRM; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, NC 27599, USA.; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211, Kuopio, Finland.; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA., East MP; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, NC 27599, USA., Laitinen T; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211, Kuopio, Finland., Alamillo-Ferrer C; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA., Hartikainen E; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211, Kuopio, Finland., Wells CI; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA., Axtman AD; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA., Drewry DH; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA., Tizzard GJ; UK National Crystallography Service, School of Chemistry, University of Southampton, Highfield Campus, Southampton, SO17 1BJ, UK., Poso A; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211, Kuopio, Finland., Willson TM; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA., Johnson GL; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, NC 27599, USA.; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

Publikováno v: BioRxiv : the preprint server for biology [bioRxiv] 2023 Dec 28. Date of Electronic Publication: 2023 Dec 28.