Kyle A. Emmitte, PhD
Professor & Chair, Department of Pharmaceutical Sciences
Education & Experience:
I received a BS in chemistry from Texas A&M University in 1996 and a PhD in Organic Chemistry from the University of North Carolina at Chapel Hill in 2001. I joined the Oncology Medicinal Chemistry group at GlaxoSmithKline in RTP, North Carolina in 2002. While at GSK, I was a member of multiple interdisciplinary teams focused on the discovery of novel small molecule ATP-competitive kinase inhibitors for the treatment of cancer. In 2008, I joined the Vanderbilt University Medical Center as Research Assistant Professor and the Vanderbilt Center for Neuroscience Drug Discovery as Associate Director of Medicinal Chemistry. While at Vanderbilt, I led several research efforts directed toward the design of novel small molecule allosteric modulators of G-protein coupled receptors for the treating disorders of the central nervous system. I joined the faculty of the UNT System College of Pharmacy as Associate Professor in July 2015. In September 2018, I was promoted to Professor with tenure and accepted the position as Chair of the Department of Pharmaceutical Sciences.
Teaching Areas & Interests:
During more than eighteen years in academic and industrial drug discovery research, I have directly mentored more than twenty different scientists of all education levels. At the UNT Health Science Center, my didactic teaching is mainly in the Doctor of Pharmacy program, specifically covering medicinal chemistry and pharmacology portions in three Integrated Pharmacotherapy (IPT) courses: Neurology and Psychiatry (PHAR 7353), Hematology, Oncology, and Transplant (PHAR 7361), and Musculoskeletal, Connective Tissues, and Rheumatologic Diseases (PHAR 7262). I also teach several sessions on cancer and drug discovery within the Introduction to Pharmacogenetics, Pharmacogenomics, and Personalized Medicine course (PHAR 7322) as well as multiple sessions on physiochemical properties in Pharmaceutics I (PHAR 7313). I am also Co-Course directing and teaching several sessions in a new online elective course entitled Overview of Modern Drug Discovery and Development that is scheduled to launch in Spring 2021. Finally, I teach sessions on medicinal chemistry and drug discovery in our graduate level course, Principles of Drug Discovery and Development (PSPT 6400).
Professional Activities & Awards:
In both 2018 and 2019, I received the Pharmaceutical Sciences Professor of the Year Award from the UNT System College of Pharmacy Student Government Association. I am a member of the American Chemical Society, American Association of Colleges of Pharmacy, American Association of Pharmaceutical Scientists and routinely serve as a reviewer for several scientific journals within the fields of medicinal chemistry and drug discovery. In 2014−2015, I organized and chaired a symposium entitled Small Molecule Approaches to Autism Spectrum Disorder Therapy for the 249th National Meeting of the American Chemical Society (ACS) in Denver, Colorado. The symposium was selected for a feature story and was published (April 27, 2015) in Chemical & Engineering News, the weekly magazine published by the ACS and made available to its more than 150K members. In 2014, the Vanderbilt Center for Technology Transfer & Commercialization selected our mGlu2 and mGlu3 NAM work as one of the 10 Cool Inventions from 2014. In 2008, I received a GSK Silver Award for project and chemistry team leadership leading to the discovery of GSK1904529, an IGF-1R clinical candidate. In 2004, I received the GSK Exceptional Science Award for sustained and key contributions to the discovery of GSK461364, a PLK1 inhibitor that advanced to clinical trials in cancer patients.
My primary research interests encompass areas related to the design and optimization of biologically active small molecules to serve as in vivo probes, drug discovery leads, and optimized preclinical compounds. I currently have active collaborations on projects across a variety of therapeutic areas, including epilepsy, autism spectrum disorders, obesity, melanoma, and glaucoma. By nature, my work is highly collaborative and engages the areas of medicinal chemistry, molecular pharmacology, in vivo biology, and drug metabolism. To date, I am an author on 60 published peer-reviewed publications, including 23 as corresponding author. I am also an inventor on 20 issued U.S. patents. Portions of my recent research have been funded by the National Institute of Mental Health (R01 MH099269) and National Institute of Neurological Disorders and Stroke (R21 NS109521 and R33 NS109521).
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5
Discovery of N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolin-amide (VU0424238): A novel negative allosteric modulator of metabotropic glutamate receptor subtype 5 selected for clinical evaluation.
Design of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as selective negative allosteric modulators of metabotropic glutamate receptor subtype 2.
Discovery of a selective and CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 with antidepressant and anxiolytic activity in rodents.
Complete List of Publications: