Gunda I. Georg is a chemist who is currently the Professor and Head of the Department of Medicinal Chemistry, [1] Regents Professor, [2] McKnight Presidential Chair, Robert Vince Endowed Chair at University of Minnesota and a former Co-Editor-in-Chief of American Chemical Society's Journal of Medicinal Chemistry . [3] Her research interests are total synthesis and semisynthesis as well as evaluating biologically active agents. [4] A cited expert in her field, [5] she was elected to the American Association for the Advancement of Science in 1996 [6] and inducted in the Medicinal Chemistry Hall of Fame in 2017. [7] In 2019, she was announced as the 2020 winner and first woman to receive the Alfred Burger Award in Medicinal Chemistry (established by GlaxoSmithKline, now sponsored by Gilead [8] ). [9] She along with chemists, Shameem Syeda and Gustavo Blanco, are leading researchers in male contraception. [10] Dr Georg also works with her research groups to conduct research on Alzheimer's disease, epilepsy and cancer experimental therapeutics. [11]
She earned her B.S. in 1975 and Ph.D. in 1980 from Philipps Universitat Marburg. [12]
Georg is the Principal Investigator for a National Institutes of Health Center grant [13] for the Contraceptive Discovery, Development and Behavioral Research Center funded from 2017 to 2021. The grant work is in five interdisciplinary groups that are working on the discovery and development of non-hormonal male contraceptive agents and the investigation of contraceptive use. [14]
Georg's work is described in over 250 peer-reviewed publications [15] and she holds a number of patents.
She co-authored a book with Lednicer and Mitscher (RIP). Her medical contributions include polishing off Gamendazole, Lonidamine and Pregnenolyne derivatives.
Isatin, also known as tribulin, is an organic compound derived from indole with formula C8H5NO2. The compound was first obtained by Otto Linné Erdman and Auguste Laurent in 1840 as a product from the oxidation of indigo dye by nitric acid and chromic acids.
A bromodomain is an approximately 110 amino acid protein domain that recognizes acetylated lysine residues, such as those on the N-terminal tails of histones. Bromodomains, as the "readers" of lysine acetylation, are responsible in transducing the signal carried by acetylated lysine residues and translating it into various normal or abnormal phenotypes. Their affinity is higher for regions where multiple acetylation sites exist in proximity. This recognition is often a prerequisite for protein-histone association and chromatin remodeling. The domain itself adopts an all-α protein fold, a bundle of four alpha helices each separated by loop regions of variable lengths that form a hydrophobic pocket that recognizes the acetyl lysine.
François Diederich was a Luxembourgian chemist specializing in organic chemistry.
Dale Lester Boger is an American medicinal and organic chemist and former chair of the Department of Chemistry at The Scripps Research Institute in La Jolla, CA.
Monoamine oxidase B, also known as MAO-B, is an enzyme that in humans is encoded by the MAOB gene.
The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it.
Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the GRM4 gene.
Combretastatin A-4 is a combretastatin and a stilbenoid. It can be isolated from Combretum afrum, the Eastern Cape South African bushwillow tree or in Combretum leprosum, the mofumbo, a species found in Brazil.
Bruce D. Roth is an American organic and medicinal chemist who trained at Saint Joseph's College, Iowa State University and the University of Rochester, and, at the age of 32, discovered atorvastatin, the statin-class drug sold as Lipitor that would become the largest-selling drug in pharmaceutical history. His honours include being named a 2008 Hero of Chemistry by the American Chemical Society, and being chosen as the Perkin Medal awardee, the highest honour given in the U.S. chemical industry, by the Society of Chemical Industry, American section in 2013.
Philip Salvatore Portoghese is an American medicinal chemist who has made notable contributions to the design and synthesis of ligands targeting opioid receptors. He is a Distinguished Professor of Medicinal Chemistry at the University of Minnesota, Twin Cities. He also served as the Editor-in-chief of the Journal of Medicinal Chemistry from 1972 to 2012, when the job was taken on by his departmental colleague, Gunda I. Georg, who shares the Editor-in-chief position with Shaomeng Wang at the University of Michigan.
Triptolide is a diterpenoid epoxide which is produced by the thunder god vine, Tripterygium wilfordii. It has in vitro and in vivo activities against mouse models of polycystic kidney disease and pancreatic cancer, but its physical properties and severe toxicity limit its therapeutic potential. Consequently, a synthetic water-soluble prodrug, minnelide, is being studied clinically instead.
Bromodomain-containing protein 9 is a protein that in humans is encoded by the BRD9 gene.
Peter Wipf is a distinguished university professor of chemistry at the University of Pittsburgh. His research interests focus on the total synthesis of natural products, the discovery of new transformations of strained molecules, and the development of new pharmaceuticals. He is a Fellow of the Royal Society of Chemistry (RSC), the American Association for the Advancement of Science (AAAS), and the American Chemical Society (ACS).
James Inglese is an American biochemist, the director of the Assay Development and Screening Technology laboratory at the National Center for Advancing Translational Sciences, a Center within the National Institutes of Health. His specialty is small molecule high throughput screening. Inglese's laboratory develops methods and strategies in molecular pharmacology with drug discovery applications. The work of his research group and collaborators focuses on genetic and infectious disease-associated biology.
Michal Hocek is a Czech chemist. He is a group leader at the Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences and a professor of organic chemistry at Charles University in Prague. He specializes in the chemistry and chemical biology of nucleosides, nucleotides, and nucleic acids.
Barry Victor Lloyd Potter MAE FMedSci is a British chemist, who is Professor of Medicinal & Biological Chemistry at the University of Oxford, Wellcome Trust Senior Investigator and a Fellow of University College, Oxford.
3CLpro-1 is an antiviral drug related to rupintrivir which acts as a 3CL protease inhibitor and was originally developed for the treatment of human enterovirus 71. It is one of the most potent of a large series of compounds developed as inhibitors of the viral enzyme 3CL protease, with an in vitroIC50 of 200 nM. It also shows activity against coronavirus diseases such as SARS and MERS, and is under investigation as a potential treatment agent for the viral disease COVID-19.
Katherine Seley-Radtke is an American medicinal chemist who specializes in the discovery and design of novel nucleoside or nucleotide based enzyme inhibitors that may be used to treat infections or cancer. She has authored over 90 peer-reviewed publications, is an inventor of five issued US patents, and is a professor in the department of chemistry and biochemistry at the University of Maryland, Baltimore County. Her international impact includes scientific collaborations, policy advising and diplomatic appointments in biosecurity efforts.
Huprine X is a synthetic cholinergic compound developed as a hybrid between the natural product Huperzine A and the synthetic drug tacrine. It is one of the most potent reversible inhibitors of acetylcholinesterase known, with a binding affinity of 0.026nM, as well as showing direct agonist activity at both nicotinic and muscarinic acetylcholine receptors. In animal studies it has nootropic and neuroprotective effects, and is used in research into Alzheimer's disease, and although huprine X itself has not been researched for medical use in humans, a large family of related derivatives have been developed.
YM-254890 is a macrolide antibiotic derived from Chromobacterium species. It is used as a pharmacological research compound which acts as a selective inhibitor of Gq mediated signalling. However the claimed selectivity for Gq has been disputed.