Largazole: from discovery to broad-spectrum therapy.

Natural Product Reports
J Hong, Hendrik Luesch

Abstract

The cyclic depsipeptide largazole from a cyanobacterium of the genus Symploca is a marine natural product with a novel chemical scaffold and potently inhibits class I histone deacetylases (HDACs). Largazole possesses highly differential growth-inhibitory activity, preferentially targeting transformed over non-transformed cells. The intriguing structure and biological activity of largazole have attracted strong interest from the synthetic chemistry community to establish synthetic routes to largazole and to investigate its potential as a cancer therapeutic. This Highlight surveys recent advances in this area with a focus on the discovery, synthesis, target identification, structure-activity relationships, HDAC8-largazole thiol crystal structure, and biological studies, including in vivo anticancer and osteogenic activities.

References

Sep 25, 2003·International Journal of Cancer. Journal International Du Cancer·Hideki KawaiHava Karsenty Avraham
Mar 26, 2004·The Prostate·Kalipso HalkidouCraig N Robson
Jul 13, 2004·Annals of the New York Academy of Sciences·Svetlana V Ukraintseva, Anatoly I Yashina
May 4, 2005·Cancer Research·Angelo AgathanggelouFarida Latif
Aug 28, 2007·Journal of Clinical Pathology·Katsuyoshi IshihamaWataru Kimura
Aug 30, 2007·Critical Reviews in Eukaryotic Gene Expression·Eric D JensenJennifer J Westendorf
Jan 22, 2008·Journal of the American Chemical Society·Kanchan TaoriHendrik Luesch
May 30, 2008·Journal of the American Chemical Society·Yongcheng YingHendrik Luesch
Jul 18, 2008·Angewandte Chemie·Tobias SeiserNicolai Cramer
Jul 23, 2008·Journal of the American Chemical Society·Albert BowersRobert M Williams
Jan 30, 2009·Natural Product Reports·Isao Fujii
Feb 3, 2009·Progress in Molecular and Subcellular Biology·Shin-ya Saito
Feb 6, 2009·Journal of the American Chemical Society·Albert A BowersJames E Bradner
May 28, 2009·Journal of Gynecologic Oncology·Ke Long JinJoo-Hyun Nam
Jul 2, 2010·Natural Product Reports·Jonathan C Morris, Andrew J Phillips
Aug 27, 2010·The Journal of Pharmacology and Experimental Therapeutics·Yanxia LiuHendrik Luesch
Oct 12, 2010·Chemistry : a European Journal·Jason C Kwan, Hendrik Luesch
Oct 30, 2010·Current Opinion in Biotechnology·Joshawna K NunneryWilliam H Gerwick
Nov 10, 2010·Journal of Asian Natural Products Research·Qiong XiaoPing Xie
Jan 27, 2011·Cancer Research·Arkaitz CarracedoPier Paolo Pandolfi
Jun 15, 2011·ACS Medicinal Chemistry Letters·Su-Ui LeeSeong Hwan Kim
Jul 28, 2011·Journal of the American Chemical Society·Kathryn E ColeDavid W Christianson
Sep 3, 2011·Future Medicinal Chemistry·Rana Montaser, Hendrik Luesch
Sep 23, 2011·Journal of Medicinal Chemistry·Pravin BhansaliL M Viranga Tillekeratne
Apr 1, 2011·Expert Opinion on Drug Discovery·Florian Thaler, Saverio Minucci

❮ Previous
Next ❯

Citations

Sep 11, 2013·Journal of Natural Products·Christopher C ThornburgKerry L McPhail
Mar 25, 2014·Marine Drugs·Mingming YuHendrik Luesch
Jun 26, 2014·Cancer Letters·Michael SchnekenburgerMarc Diederich
Dec 20, 2015·Journal of Chemical Information and Modeling·Flavio Ballante, Garland R Marshall
May 29, 2013·Drug Discovery Today·Lik Tong Tan
Nov 18, 2015·Organic Letters·Olugbeminiyi O FadeyiRalph Robinson
Sep 10, 2014·European Journal of Medicinal Chemistry·Pravin BhansaliL M Viranga Tillekeratne
Jul 23, 2016·Cell Chemical Biology·Alex R MaolanonChristian A Olsen
Jul 28, 2016·Accounts of Chemical Research·Philipp Koschker, Bernhard Breit
Jan 13, 2015·Natural Product Reports·Lilibeth A Salvador-Reyes, Hendrik Luesch
Mar 21, 2018·International Journal of Molecular Sciences·Hee Kyoung KangYoonkyung Park
Nov 4, 2016·Chemical Communications : Chem Comm·Stacy L Capehart, Erin E Carlson
Oct 8, 2014·Angewandte Chemie·Timothy A HillDavid P Fairlie
Jan 13, 2015·ChemMedChem·Shuai Tan, Zhao-Peng Liu
Mar 27, 2019·Journal of Biomolecular Structure & Dynamics·Varun DewakerYenamandra S Prabhakar
Jan 7, 2014·Natural Product Reports·John W BluntMichèle R Prinsep
Oct 20, 2018·Current Medicinal Chemistry·Loredana CappellacciRiccardo Petrelli
Oct 18, 2016·Chembiochem : a European Journal of Chemical Biology·Alex R MaolanonChristian A Olsen
Aug 6, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Zachary BarryTimothy W Corson
Dec 12, 2018·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Santiago LascanoPaola B Arimondo
Jul 14, 2019·Clinical Epigenetics·Yorick JanssensBart De Spiegeleer
Apr 23, 2020·International Journal of Oncology·Min WangGuang-Biao Zhou
Sep 10, 2020·Frontiers in Pharmacology·Sergi Herve AkoneRolf Müller
May 7, 2013·Natural Product Reports·Zhong Jin
Jan 31, 2014·Chemistry : a European Journal·Christoph SchotesBernhard Breit
May 14, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lik Tong Tan, Ma Yadanar Phyo
Oct 20, 2020·Protein Science : a Publication of the Protein Society·Diego A Alonzo, T Martin Schmeing
Jul 29, 2019·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Xiao LiangHendrik Luesch

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.