Medicinal Chemistry and Virology Together in the Service of Human Health: In Honor of Prof. Dr. Erik De Clercq on the Occasion of His 85th Birthday
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 31 December 2026 | Viewed by 120
Editors
Interests: arthropod-borne viruses as causative agent of severe diseases of human and animals, especially flavivirues transmitted by ticks; interaction of tick-borne flaviviruses with host cells, innate immunity against flaviviruses; structural and non-structural proteins of flaviviruses, especially tick-borne Encephalitis virus; ticks as vectors of flaviviruses and borrelia spirochetes; vaccines agains ticks and tick transmitted pathogens
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2. Institute of Parasitology, Biology Centre of the Czech Academy of Sciences, 37005 Ceske Budejovice, Czech Republic
3. Veterinary Research Institute, 62100 Brno, Czech Republic
Interests: tick-borne encephalitis; arboviruses; pathogenesis; antivirals; vaccines
Special Issues, Collections and Topics in MDPI journals
Interests: genome-wide diversity; coevolution and interaction of HIV, HBV and HCV; the development of antiviral drugs and vaccines
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
This Special Issue of Molecules is dedicated to Prof. Dr. Erik De Clercq on the occasion of his 85th anniversary. The Guest Editor team, along with the Editors of Molecules, invite scientists to join us in celebrating Prof. Dr. Erik De Clercq’s exceptional achievements by contributing original research articles as well as reviews.
Prof. Dr. Erik De Clercq was born on 28 March 1941 in Dendermonde (Belgium) and later graduated as Medical Doctor (MD) in 1966 and Philosophical Doctor (PhD) in 1972. He has been a Full Professor at the Faculty of Medicine (KU Leuven) since his appointment in 1977. He spent two years at Stanford University (1968–1970), and the rest of his career at the Rega Institute for Medical Research (KU Leuven). Prof. De Clercq holds an Honorary Doctorate from the Universities of Ghent, Athens, Ferrara, Shandong, Prague (Charles), Česke Budějovice, Tours, and Hull and is an honorary citizen of the town of Hamme (Belgium). He was named inventor of the year in 2008 (EU), and Laureate of the Dr. Paul Janssen Prize in 2010. He is best known for his co-invention (together with Dr. Antonín Holý) of the anti-HIV drug, tenofovir. Prof. De Clercq has taught courses in Microbiology (Virology) and Biochemistry at KU Leuven and KU Leuven Campus, Kortrijk. Since 2006, he has been serving as Emeritus Professor at KU Leuven, but has continued teaching, since 2007 until today, the course on “Biochemistry at the Service of Medicine” to Bachelor’s and Master’s students at the Universities of Česke Budějovice (Budweis) and Linz.
Prof. Erik De Clercq has contributed to the development of seven antiviral drugs: tenofovir disoproxil fumarate (Viread®) for HIV and HBV treatment, tenofovir alafenamide (Vemlidy®) for HIV and HBV treatment, brivudine (Zostex®) for HSV-1 and VZV treatment, valacyclovir (Valtrex ®) for HSV and VZV treatment, adefovir dipivoxil (Hepsera®) for HBV treatment, stavudine (Zerit®) for HIV treatment, and cidofovir (Vistide®) for treating HCMV retinitis in AIDS patients. In addition to the above antiviral drugs, his contributions include two anti-cancer drugs: rabacfosadine (Tanovea®-CA1) for canine lymphoma and plerixafor (Mozobil®) for multiple myeloma and non-Hodgkin’s lymphoma. Since the beginning of his career in 1957, Prof. Erik De Clercq has contributed more than 2900 scientific publications and 100 patents, mostly in the field of antiviral research.
Highlights in the scientific career of (Prof. Dr.) Erik De Clercq include:
- In 1968, the discovery of several inducers of interferon (e.g., polyacrylic acid).
- In 1975, the inhibition of the murine reverse transcriptase by suramin, the first compound ever to be demonstrated as an inhibitor of HIV infection both in vitro (citation of text from Mitsuya et al. on E. De Clercq’s article in Cancer Letters) and in vivo (humans).
- In 1979, the discovery of BVDU as a potent and selective anti-HSV-1 agent, later marketed globally for the treatment of VZV infections (herpes zoster), following the original report of E. De Clercq et al.
- In 1978, the discovery of DHPA, together with acyclovir, the first acyclic nucleoside found to exhibit antiviral activity.
- In 1980, the cloning and expression of human β-interferon and elucidation of its primary structure.
- In 1982, the identification of the amino acid esters of acyclovir from which the valine ester (valacyclovir) would become its successor on the worldwide market.
- In 1986, the discovery of acyclic nucleoside phosphonates (i.e., HPMPA, PMEA) as a new class of broad-spectrum anti-DNA virus agents.
- In 1987, the discovery of d4T (2’,3’-dideoxy-2’,3’-didehydro thymidine), later marketed as stavudine, for the treatment of HIV infections.
- In 1989 and 1990, the discovery of NNRTIs (non-nucleoside reverse transcriptase inhibitors) with not only one but two prototypes, the HEPT and TIBO derivatives. The latter would eventually lead to the development of rilpivirine for the drug market.
- In 1993, the discovery of PMPA, which later became known as tenofovir, which would become the most popular anti-HIV drug worldwide for the treatment of HIV infections.
- In 1998, tenofovir was derivatized to its prodrug, tenofovir disoproxil fumarate (TDF); in 2005, a new prodrug of tenofovir, tenofovir alafenamide (TAF), was developed, and TDF and TAF have been marketed worldwide for the treatment of HIV and hepatitis B virus (HBV) infections.
- Tenofovir (as TDF or TAF), in combination with emtricitabine, has become the only compound in the world to be used in the prophylaxis (prevention) of HIV infections (commonly referred to as PrEP: pre-exposure prophylaxis).
- As of 2020, 15 marketed drugs containing tenofovir (TDF or TAF) have become available all over the world.
- In 2000, a new nucleoside analog, Cf-1743, was discovered, which is even more potent than BVDU and yields great potential as a valine ester (fermavir, FV-100) for the treatment of VZV infections.
- Since 2018, a new phosphonate analog (derivatized from PMEG) has become available for the treatment of (malignant) lymphomas in dogs (Tanovea®).
- Originally described as an anti-HIV agent in 1992 (paper sponsored by the Nobel Prize winner Mx Perutz) and 1994, a bicyclam derivative, AMD-3100 (plerixafor), has been found to be effective as a stem cell mobilizer (Mozobil®), and has been licensed for autologous transplantation in patients with multiple myeloma or non-Hodgkin’s lymphoma.
Prof. Dr. Libor Grubhoffer
Prof. Dr. Daniel Růžek
Prof. Dr. Guangdi Li
Guest Editors
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Keywords
- antiviral agents
- medicinal chemistry
- virology
- nucleoside/nucleotide analogs
- HIV therapeutics
- drug development
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