Antonín Holý
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Antonín Holý (1 September 1936 – 16 July 2012) was a pioneering
Czech Czech may refer to: * Anything from or related to the Czech Republic, a country in Europe ** Czech language ** Czechs, the people of the area ** Czech culture ** Czech cuisine * One of three mythical brothers, Lech, Czech, and Rus' Places * Czech, ...
scientist. He specialised in the field of
chemistry Chemistry is the science, scientific study of the properties and behavior of matter. It is a natural science that covers the Chemical element, elements that make up matter to the chemical compound, compounds made of atoms, molecules and ions ...
and cooperated on the development of important
antiretroviral drugs The management of HIV/AIDS normally includes the use of multiple antiretroviral drugs as a strategy to control HIV infection. There are several classes of antiretroviral agents that act on different stages of the HIV life-cycle. The use of multipl ...
used in the treatment of
HIV The human immunodeficiency viruses (HIV) are two species of ''Lentivirus'' (a subgroup of retrovirus) that infect humans. Over time, they cause acquired immunodeficiency syndrome (AIDS), a condition in which progressive failure of the immune ...
and
hepatitis B Hepatitis B is an infectious disease caused by the ''Hepatitis B virus'' (HBV) that affects the liver; it is a type of viral hepatitis. It can cause both acute and chronic infection. Many people have no symptoms during an initial infection. Fo ...
. He was involved in the creation of the most effective drug (as of early 2009) in the treatment of
AIDS Human immunodeficiency virus infection and acquired immunodeficiency syndrome (HIV/AIDS) is a spectrum of conditions caused by infection with the human immunodeficiency virus (HIV), a retrovirus. Following initial infection an individual m ...
. Antonín Holý is the author of more than 450 papers, 400 scientific discoveries and holds 60 patents. With more than 400 discoveries to his credit, his work has affected millions of people with viral diseases such as HIV/AIDS and hepatitis B and many other viral diseases. In 2008 he received an Honorary Professorship at the
University of Manchester , mottoeng = Knowledge, Wisdom, Humanity , established = 2004 – University of Manchester Predecessor institutions: 1956 – UMIST (as university college; university 1994) 1904 – Victoria University of Manchester 1880 – Victoria Univer ...
's School of Chemistry.


Scientific career

Born in
Prague Prague ( ; cs, Praha ; german: Prag, ; la, Praga) is the capital and largest city in the Czech Republic, and the historical capital of Bohemia. On the Vltava river, Prague is home to about 1.3 million people. The city has a temperate ...
,
Czechoslovakia , rue, Чеськословеньско, , yi, טשעכאסלאוואקיי, , common_name = Czechoslovakia , life_span = 1918–19391945–1992 , p1 = Austria-Hungary , image_p1 ...
, Antonín Holý studied
organic chemistry Organic chemistry is a subdiscipline within chemistry involving the scientific study of the structure, properties, and reactions of organic compounds and organic materials, i.e., matter in its various forms that contain carbon atoms.Clayden, J.; ...
from 1954 to 1959 at the Faculty of Science of
Charles University in Prague Charles University ( cs, Univerzita Karlova, UK; la, Universitas Carolina; german: Karls-Universität), also known as Charles University in Prague or historically as the University of Prague ( la, Universitas Pragensis, links=no), is the oldest an ...
. From 1960 he trained at the Institute of Organic Chemistry and Biochemistry (IOCB) of the
Czechoslovak Academy of Sciences The Czechoslovak Academy of Sciences (Czech: ''Československá akademie věd'', Slovak: ''Česko-slovenská akadémia vied'') was established in 1953 to be the scientific center for Czechoslovakia. It was succeeded by the Czech Academy of Science ...
in Prague and had been a researcher there since 1963. He became the Institute's lead scientist in 1967, and from 1983 headed its working group for
nucleic acids Nucleic acids are biopolymers, macromolecules, essential to all known forms of life. They are composed of nucleotides, which are the monomers made of three components: a 5-carbon sugar, a phosphate group and a nitrogenous base. The two main clas ...
. In 1987 he became chief of the Department of Nucleic Acid Chemistry 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 The Rega Institute for Medical Research is a Belgian scientific establishment that is part of the Catholic University of Leuven (Leuven) in central Belgium. The Rega Institute is an interfacultary biomedical research institute of the Catholic Univ ...
at the
Catholic University of Leuven University of Leuven or University of Louvain (french: Université de Louvain, link=no; nl, Universiteit Leuven, link=no) may refer to: * Old University of Leuven (1425–1797) * State University of Leuven (1817–1835) * Catholic University of ...
,
Belgium Belgium, ; french: Belgique ; german: Belgien officially the Kingdom of Belgium, is a country in Northwestern Europe. The country is bordered by the Netherlands to the north, Germany to the east, Luxembourg to the southeast, France to th ...
. His key contribution is the synthesis of
nucleotide analogues Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drugs used to treat HIV infection or AIDS, and in some cases hepatitis B. RTIs inhibit activity of reverse transcriptase, a viral DNA polymerase that is required for replicatio ...
, synthetic mimetics of the building blocks of
RNA Ribonucleic acid (RNA) is a polymeric molecule essential in various biological roles in coding, decoding, regulation and expression of genes. RNA and deoxyribonucleic acid ( DNA) are nucleic acids. Along with lipids, proteins, and carbohydra ...
and DNA, that have found utility as inhibitors of viral replication. These include
Tenofovir Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for preven ...
,
Adefovir Adefovir is a prescription medicine used to treat (chronic) infections with hepatitis B virus. A prodrug form of adefovir was previously called bis-POM PMEA, with trade names Preveon and Hepsera. It is an orally administered nucleotide analog reve ...
and
Cidofovir Cidofovir, brand name Vistide, is a topical or injectable antiviral medication primarily used as a treatment for cytomegalovirus (CMV) retinitis (an infection of the retina of the eye) in people with AIDS. Cidofovir was approved for medical us ...
. Although ineffective as originally synthesized by Holy because of impermeability conferred by the negative charged phosphonate, conjugation with POM and POC pro-drug moieties developed by David Farquhar at
M.D. Anderson Cancer Center The University of Texas MD Anderson Cancer Center (colloquially MD Anderson Cancer Center) is a comprehensive cancer center in Houston, Texas. It is the largest cancer center in the U.S. and one of the original three comprehensive cancer centers ...
, has made these nucleotide analogues into clinically effective drugs for the treatment of Hepatitis B (biPOM-Adefovir,
Hepsera Adefovir is a prescription medicine used to treat (chronic) infections with hepatitis B virus. A prodrug form of adefovir was previously called bis-POM PMEA, with trade names Preveon and Hepsera. It is an orally administered nucleotide analog reve ...
), and biPOC-Tenofovir
Tenofovir Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for preven ...
. Together, these drugs have made an dramatic impact for the treatment of HIV. In particular, Truvada has shown exceptionally useful in preventing HIV transmission and thus has not only helped countless HIV patients, but has in fact prevented countless other healthy individuals from contracting the disease in the first place. In 2006 the US
biopharmaceutical A biopharmaceutical, also known as a biological medical product, or biologic, is any pharmaceutical drug product manufactured in, extracted from, or semisynthesized from biological sources. Different from totally synthesized pharmaceuticals, t ...
company
Gilead Sciences Gilead Sciences, Inc. () is an American biopharmaceutical company headquartered in Foster City, California, that focuses on researching and developing antiviral drugs used in the treatment of HIV/AIDS, hepatitis B, hepatitis C, influenza, and CO ...
, under the direction of
Tomáš Cihlář Tomáš Cihlář (born 1967) is a Czech biochemist known for his role in the development of remdesivir. A specialist in virology, Cihlář holds the positions of Senior Director, Biology, and Vice-President at American pharmaceutical company Gilea ...
, and the Institute of Organic Chemistry and Biochemistry (IOCB) of the Academy of Sciences of the Czech Republic jointly established a new research center, oriented to the development of new preparations. Gilead promised the IOCB a $1.1 million donation, to fund its operations and research for 5 years. Several antiretroviral drugs based on Holý's discoveries have been licensed. In 1996, Vistide was approved for production in the
United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territorie ...
and
European Union The European Union (EU) is a supranational political and economic union of member states that are located primarily in Europe. The union has a total area of and an estimated total population of about 447million. The EU has often been des ...
.
Viread Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for preven ...
(tenofovir) was approved in the US in 2001 for the treatment of AIDS, and
Hepsera Adefovir is a prescription medicine used to treat (chronic) infections with hepatitis B virus. A prodrug form of adefovir was previously called bis-POM PMEA, with trade names Preveon and Hepsera. It is an orally administered nucleotide analog reve ...
was approved in 2003 for the treatment of hepatitis B.
Truvada Emtricitabine/tenofovir, sold under the brand name Truvada among others, is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS. It contains the antiretroviral medications emtricitabine and tenofovir disopro ...
, a combination of Viread and
emtricitabine Emtricitabine (commonly called FTC, systematic name 2',3'-dideoxy-5-fluoro-3'-thiacytidine), with trade name Emtriva (formerly Coviracil), is a nucleoside reverse-transcriptase inhibitor (NRTI) for the prevention and treatment of HIV infection in ...
, was approved in 2006 for use in the USA.


Death

Holý had retired a year before his death and died of an unspecified cause, aged 75, on 16 July 2012. A statement from the IOCB called his death "an immense loss". His death occurred two months after the U.S.
Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...
(FDA) approved
Truvada Emtricitabine/tenofovir, sold under the brand name Truvada among others, is a fixed-dose combination antiretroviral medication used to treat and prevent HIV/AIDS. It contains the antiretroviral medications emtricitabine and tenofovir disopro ...
for treating HIV.


Awards and honours

* 1984 State Prize for Chemistry (''Acyklická analoga nukleosidů a nukleotidů'') * 1998 Honor plaque: Nucleic Acids Chemistry journal * 1999 Hanuš's Medal of the '' Czech Chemical Society''; Honorary doctorate of the Palacký University in
Olomouc Olomouc (, , ; german: Olmütz; pl, Ołomuniec ; la, Olomucium or ''Iuliomontium'') is a city in the Czech Republic. It has about 99,000 inhabitants, and its larger urban zone has a population of about 384,000 inhabitants (2019). Located on th ...
* 2001
Descartes Prize The Descartes Prize was an annual award in science given by the European Union, named in honour of the French mathematician and philosopher, René Descartes. The prizes recognized Outstanding Scientific and Technological Achievements Resulting f ...
of the European Union; The Medal of Merit of the Czech Republic (''Za zásluhy'') I. degree * 2002 Elion Award of International Society for Antiviral Research; State Medal "''Pour merit''" * 2003 Honorary membership in the Rega Institute for Medical Research, Catholic University of Leuven, Belgium. * 2004 Award ''Praemium Bohemiae''; Medal of the Czech Academy of Sciences: ''De scientia et humanitate optime meritis'' * 2005 Honorary doctorate of the
Ghent University Ghent University ( nl, Universiteit Gent, abbreviated as UGent) is a public research university located in Ghent, Belgium. Established before the state of Belgium itself, the university was founded by the Dutch King William I in 1817, when the ...
(Belgium); The Medal of Merit of the Faculty of Science at the Charles University in Prague. * 2006 Member of the
European Academy of Sciences and Arts The European Academy of Sciences and Arts (EASA, la, Academia Scientiarum et Artium Europaea) is a transnational and interdisciplinary network, connecting about 2,000 recommended scientists and artists worldwide, including 37 Nobel Prize laure ...
(
Salzburg Salzburg (, ; literally "Salt-Castle"; bar, Soizbuag, label=Bavarian language, Austro-Bavarian) is the List of cities and towns in Austria, fourth-largest city in Austria. In 2020, it had a population of 156,872. The town is on the site of the ...
) * 2006 Honorary doctorate of the
Institute of Chemical Technology in Prague The University of Chemistry and Technology, Prague (UCT Prague; cs, Vysoká škola chemicko-technologická v Praze, VŠCHT Praha) is the largest university specializing in chemistry in the Czech Republic. Though founded in 1952, UCT Prague has or ...
* 2007 State Prize "Czech Head" (''Česká hlava'') * 2008 Honorary Professorship at the
School of Chemistry, University of Manchester The Department of Chemistry at the University of Manchester is one of the largest Departments of Chemistry in the United Kingdom, with over 600 undergraduate and more than 200 postgraduate research students. The department has comprehensive academ ...
* 2009 Honorary doctorate of the
University of South Bohemia in České Budějovice University of South Bohemia in České Budějovice ( cz, Jihočeská univerzita v Českých Budějovicích, la, Universitas Bohemiae Meridionalis Budovicensis, JU or JČU) is a public university located in the city of České Budějovice (with ...
* 2011 Silver memorial medal of the
Senate of the Parliament of the Czech Republic The Senate (), literally "Senate of the Parliament of the Czech Republic", is the upper house of the Parliament of the Czech Republic. The seat of the Senate is Wallenstein Palace in Prague. Structure The Senate has 81 members, chosen in s ...
* 2012 Silver medal of the City of Prague


See also

*
Adefovir Adefovir is a prescription medicine used to treat (chronic) infections with hepatitis B virus. A prodrug form of adefovir was previously called bis-POM PMEA, with trade names Preveon and Hepsera. It is an orally administered nucleotide analog reve ...
*
Cidofovir Cidofovir, brand name Vistide, is a topical or injectable antiviral medication primarily used as a treatment for cytomegalovirus (CMV) retinitis (an infection of the retina of the eye) in people with AIDS. Cidofovir was approved for medical us ...
*
Tenofovir Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for preven ...


References


External links

{{DEFAULTSORT:Holy, Antonin 1936 births 2012 deaths Czech chemists Gilead Sciences people Scientists from Prague Recipients of Medal of Merit (Czech Republic) Members of the European Academy of Sciences and Arts Charles University alumni Institute of Organic Chemistry and Biochemistry of the CAS