Robert Vince | |
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| Born | November 20, 1940 (age 82) Auburn, New York |
| Alma mater | SUNY, Buffalo, New York |
| Known for | Abacavir, Vince Lactam, Carbovir, Acyclovir |
Robert Vince (born November 20, 1940) is an American scientist known for his contributions to the research in the area of drug design. He is currently the director and professor at the Center for Drug Design at the Academic Health Center for the University of Minnesota.
Robert Vince was born in Auburn, New York. After graduating with a Bachelor of Science in Pharmacy in 1962, Vince joined the research group of Prof Howard J. Schaeffer at SUNY Buffalo in New York, where he obtained his doctoral degree in medicinal chemistry. He subsequently joined the University of Mississippi for a brief stint as assistant professor of medicinal chemistry. In 1967, he joined the medicinal chemistry faculty at the University of Minnesota. [1] In 2002, Vince established the Center for Drug Design within the Academic Health Center of the University of Minnesota, where he continues as director and maintains his research program. [2]
As a graduate student, Vince’s research on the design of acyclonucleosides, with Howard J. Schaeffer at SUNY Buffalo became an integral part of the discovery of anti-viral drug acyclovir. [3] Later, Prof Schaeffer continued the development of acyclovir at Burroughs Welcome & Company, with pharmacologist Gertrude B. Elion who was awarded the 1988 Nobel Prize in Medicine, in part, for the development of acyclovir. [4] Dr. Vince continued his work on antiviral drug candidates at the University of Minnesota, where he went on to develop carbocyclic nucleosides termed 'carbovirs'. This class of medicinal agents included the drug abacavir. [5] Abacavir was commercialized by GlaxoSmithKline as Ziagen for the treatment of AIDS. Sales from Ziagen have resulted in generation of more than 600 million US dollars in royalties for the University of Minnesota. [1]
His synthesis of abacavir made use of a bicyclic γ-lactam, 2-azabicyclo[2.2.1]hept-5-en-3-one, as a chemical precursor. In recognition of his contribution to the development of this field, Chemical and Engineering News gave this molecule a general name, ‘Vince lactam’ in 2003. [6] Vince lactam has since been utilized to prepare several drugs and pharmaceutical candidates. [1]
For his work, Vince has received recognition from several avenues. He was elected as the Fellow of AAAS by The American Association for the Advancement of Science in 2000. [7] He was inducted into the Medicinal Chemistry Hall of Fame of the American Chemical Society in 2007. [8] Vince was awarded Honorary Doctorate of Science Degree by his alma mater SUNY Buffalo, [9] and the prestigious Imbach Townsend Award by the International Society for Nucleosides, Nucleotides and Nucleic Acids, in 2010. [10] The same year, Minnesota Inventor’s Congress inducted him into Minnesota Inventors Hall of Fame, along with Nobel laureate Dr. Norman Borlaug (posthumously). [11] In 2011, he was inducted into Minnesota Science & Technology Hall of Fame. [12] In 2017, the New York State Senate adopted a legislative resolution commending him upon the occasion of his designation as a 2017 Inductee into the Auburn Alumni Hall of Distinction. [13] He was honored at the National Academy of Inventors (NAI) Annual Conference as an NAI Fellow in 2018, [14] and recently was selected for the Innovation Impact Case Award (2022). [15]
Guanosine (symbol G or Guo) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine can be phosphorylated to become guanosine monophosphate (GMP), cyclic guanosine monophosphate (cGMP), guanosine diphosphate (GDP), and guanosine triphosphate (GTP). These forms play important roles in various biochemical processes such as synthesis of nucleic acids and proteins, photosynthesis, muscle contraction, and intracellular signal transduction (cGMP). When guanine is attached by its N9 nitrogen to the C1 carbon of a deoxyribose ring it is known as deoxyguanosine.
Nucleosides are glycosylamines that can be thought of as nucleotides without a phosphate group. A nucleoside consists simply of a nucleobase and a five-carbon sugar whereas a nucleotide is composed of a nucleobase, a five-carbon sugar, and one or more phosphate groups. In a nucleoside, the anomeric carbon is linked through a glycosidic bond to the N9 of a purine or the N1 of a pyrimidine. Nucleotides are the molecular building blocks of DNA and RNA.
Gertrude "Trudy"Belle Elion was an American biochemist and pharmacologist, who shared the 1988 Nobel Prize in Physiology or Medicine with George H. Hitchings and Sir James Black for their use of innovative methods of rational drug design for the development of new drugs. This new method focused on understanding the target of the drug rather than simply using trial-and-error. Her work led to the creation of the anti-retroviral drug AZT, which was the first drug widely used against AIDS. Her well known works also include the development of the first immunosuppressive drug, azathioprine, used to fight rejection in organ transplants, and the first successful antiviral drug, acyclovir (ACV), used in the treatment of herpes infection.
Aciclovir (ACV), also known as acyclovir, is an antiviral medication. It is primarily used for the treatment of herpes simplex virus infections, chickenpox, and shingles. Other uses include prevention of cytomegalovirus infections following transplant and severe complications of Epstein–Barr virus infection. It can be taken by mouth, applied as a cream, or injected.
Abacavir, sold under the brand name Ziagen among others, is a medication used to treat HIV/AIDS. Similar to other nucleoside analog reverse-transcriptase inhibitors (NRTIs), abacavir is used together with other HIV medications, and is not recommended by itself. It is taken by mouth as a tablet or solution and may be used in children over the age of three months.
Vidarabine or 9-β-D-arabinofuranosyladenine (ara-A) is an antiviral drug which is active against herpes simplex and varicella zoster viruses.
An antimetabolite is a chemical that inhibits the use of a metabolite, which is another chemical that is part of normal metabolism. Such substances are often similar in structure to the metabolite that they interfere with, such as the antifolates that interfere with the use of folic acid; thus, competitive inhibition can occur, and the presence of antimetabolites can have toxic effects on cells, such as halting cell growth and cell division, so these compounds are used as chemotherapy for cancer.
Nucleoside analogues are nucleosides which contain a nucleic acid analogue and a sugar. Nucleotide analogs are nucleotides which contain a nucleic acid analogue, a sugar, and a phosphate group with one to three phosphates.
Richard Bruce Silverman is the Patrick G. Ryan/Aon Professor of Chemistry at Northwestern University. His group's main focus is basic and translational research into central nervous system disorders and cancer. He is known for the discovery of pregabalin, which is marketed by Pfizer under the brand name Lyrica.
Charon Robin Ganellin FRS is a British medicinal chemist, and Emeritus Smith Kline and French Professor of Medicinal Chemistry, at University College London.
Vince lactam is the commercial name given to the bicyclic molecule γ-lactam 2-azabicyclo[2.2.1]hept-5-en-3-one. This lactam is a versatile chemical intermediate used in organic and medicinal chemistry. It is used as a synthetic precursor for three drugs. It is named after Robert Vince who has used the structural features of this molecule for the preparation of carbocyclic nucleosides. Vince's work with this lactam eventually led to his synthesis of abacavir. Peramivir synthesis is also dependent on Vince lactam starting material.
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.
The ProTide technology is a prodrug approach used in molecular biology and drug design. It is designed to deliver nucleotide analogues into the cell. It was invented by Professor Chris McGuigan in the early 1990s. They form a critical part of the anti-viral drugs: sofosbuvir, tenofovir alafenamide and remdesivir.
Carbocyclic nucleosides are nucleoside analogues in which a methylene group has replaced the oxygen atom of the furanose ring. These analogues have the nucleobase attached at a simple alkyl carbon rather than being part of a hemiaminal ether linkage. As a result, they have increased chemical stability. They also have increased metabolic stability because they are unaffected by phosphorylases and hydrolases that cleave the glycosidic bond between the nucleobase and furanose ring of nucleosides. They retain many of the biological properties of the original nucleosides with respect to recognition by various enzymes and receptors.
Ann E. Weber is the Senior Vice President for Drug Discovery at Kallyope Inc. in New York City. She previously worked with Merck Research Laboratories (MRL), joining the company in 1987 and retiring from the position of Vice President for Lead Optimization Chemistry in 2015. She has helped develop more than 40 drug candidates including FDA-approved treatments for Type 2 diabetes. She has received a number of awards, including the Perkin Medal (2017) and has been inducted into the ACS Division of Medicinal Chemistry’s MEDI Hall of Fame.
Gunda I. Georg is a chemist who is currently the Professor and Head of the Department of Medicinal Chemistry, Regents Professor, 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. Her research interests are total synthesis and semisynthesis as well as evaluating biologically active agents. A cited expert in her field, she was elected to the American Association for the Advancement of Science in 1996 and inducted in the Medicinal Chemistry Hall of Fame in 2017. In 2019, she was announced as the 2020 winner and first woman to receive the Alfred Burger Award in Medicinal Chemistry. She along with chemists, Shameem Syeda and Gustavo Blanco, are leading researchers in male contraception. Dr Georg also works with her research groups to conduct research on Alzheimer's disease, epilepsy and cancer experimental therapeutics.
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.
Janet Rideout is an organic chemist and one of the scientists who discovered that azidothymidine (AZT) could be used as an antiretroviral agent to treat Human Immunodeficiency Virus (HIV). She also played a key role in the development of acyclovir, the first effective treatment for herpes simplex virus.
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 & Biochemistry at the University of Maryland, Baltimore County. Her international impact includes scientific collaborations, policy advising and diplomatic appointments in biosecurity efforts.
Sir William Alexander Denny is a New Zealand medicinal chemist, noted for his work investigating drugs for the treatment of cancer.