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Antonín Holý

Czech chemist (1936–2012) From Wikipedia, the free encyclopedia

Antonín Holý (1 September 1936 – 16 July 2012) was a Czech medicinal chemist known for his research on acyclic nucleoside phosphonates (ANPs), an important class of antiviral nucleotide analogues.[1] He spent most of his scientific career at the Institute of Organic Chemistry and Biochemistry in Prague, where he served as director from 1994 to 2002.[2] In a long-term collaboration with virologist Erik De Clercq, Holý synthesized antiviral compounds including Cidofovir, Adefovir and Tenofovir.[3]

Born(1936-09-01)September 1, 1936
DiedJuly 16, 2012(2012-07-16) (aged 75)
KnownforAntiretroviral drugs used in the treatment of HIV
Quick facts Born, Died ...
Antonín Holý
Born(1936-09-01)September 1, 1936
DiedJuly 16, 2012(2012-07-16) (aged 75)
EducationCharles University in Prague
Known forAntiretroviral drugs used in the treatment of HIV
SpouseLudmila Holá
Scientific career
FieldsChemist
WorkplacesCzechoslovak Academy of Sciences (1960 – 1992)
Academy of Sciences of the Czech Republic (1992 – 2002)
Doctoral students
Michal Hocek
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These compounds were subsequently developed into medicines used against Cytomegalovirus infections, Hepatitis B and HIV/AIDS. Tenofovir also became a component of combination therapies used for both HIV treatment and prevention.[4] Holý's work has been credited with improving or extending the lives of millions of people with viral diseases worldwide.[5] Over his career, he co-authored around 600 scientific publications and held more than 60 patents.[6]

Scientific career

Born in Prague, Czechoslovakia, Antonín Holý studied organic chemistry from 1954 to 1959 at the Faculty of Mathematics and Physics of Charles University in Prague. From 1960 he joined the Institute of Organic Chemistry and Biochemistry (IOCB) of the Czechoslovak Academy of Sciences in Prague and had been a researcher there since 1963. He became the institute's lead scientist in 1967, and from 1983 headed its nucleic acids chemistry group. In 1987 he became head of the Bioorganic Chemistry Department and from 1994 to 2002 he was head of the IOCB.

Since 1976 he had collaborated on the development of new antiretroviral drugs with Erik De Clercq of the Rega Institute for Medical Research at the Catholic University of Leuven, Belgium.[7]

His key contribution is the synthesis of nucleotide analogues, synthetic mimetics of the building blocks of RNA and DNA, that have found utility as inhibitors of viral replication. Clinically important compounds included Tenofovir, Adefovir and Cidofovir, which were subsequently developed into antiviral medicines.[8]

Tenofovir became an important component of combination therapies for HIV treatment and, in combination with Emtricitabine, of Pre-exposure prophylaxis (PrEP) for HIV prevention.

In 2006, IOCB and Gilead Sciences launched the Gilead Sciences Research Centre, a five-year research partnership supporting work on human diseases at the institute.[9] Under the agreement, Gilead provided $1.1 million annually for five years to support the research programme.[10]

Several antiviral drugs developed from this research were later approved for clinical use. Cidofovir (Vistide) was approved in the United States in 1996 for Cytomegalovirus retinitis, followed by Tenofovir disoproxil (Viread) for HIV-1 infection in 2001 and Adefovir dipivoxil (Hepsera) for chronic hepatitis B in 2002.[11][12] In 2004, Emtricitabine and tenofovir disoproxil fumarate were combined as Truvada, which was approved for the treatment of HIV-1 infection.[13]

Death

Holý retired on 1 September 2011, his 75th birthday, and died in Prague on 16 July 2012 following a long illness. [14] On the same day, the U.S. Food and Drug Administration approved Truvada for pre-exposure prophylaxis (PrEP) to reduce the risk of HIV infection.[15][16]

Awards and honours

See also

References

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