Marie Cote, Deputy Editor – Page 3 – RSC Medicinal Chemistry Blog

Author Archive

Epigenetics: a highly promising source of new drug targets

12 Dec 2011

As an introduction to the web theme issue on Epigenetics published in MedChemComm (guest-edited by Dr Mark Bunnage – Pfizer – and Professor Rasmus Prætorius Clausen -University of Copenhagen), Nessa Carey (Head of Epigenetics ERDI, Pfizer) provides a concise summary of the current thinking in the ever expanding field of epigenetics.

Read Nessa’s review:
Epigenetics – an emerging and highly promising source of new drug targets
Nessa Carey
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C1MD00264C

…and view the collection of articles that makes for a timely and essential web theme issue in the emerging field of epigenetics research.

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HOT Review: Epigenetic modulators for cancer chemotherapy

21 Nov 2011

In this Hot review article Professor Patrick Woster and a team of international collaborators provide insights into the design, synthesis and biological activity of a range of chromatin remodeling enzymes inhibitors that promote the re-expression of aberrantly silenced genes of importance in human cancer.

Interested in Epigenetic therapeutics? Why not read the article now:

Polyamine-based small molecule epigenetic modulators
DOI: 10.1039/C1MD00220A, Review

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HOT: A self-immolative strategy to enhance cancer chemotherapy selectivity

04 Nov 2011

In this Hot article, scientists from France present a self-immolative dendritic glucuronide prodrug designed for the release of two doxorubicin molecules after a single triggering event.

‘While numerous glucuronide prodrugs have been studied so far, the efficiency of this targeting strategy is limited by the poor turnover of beta-glucuronidase in malignant tissues. Our novel dendritic prodrug which is programmed to release two molecules of doxorubicin after a single enzymatic activation step may permit to overcome this drawback’, the authors explain.

The biological experiments conducted have shown that this novel enzyme-responsive dendritic prodrug is twice more toxic than its monomeric counterpart against H661 lung cancer cells. It is hoped that this novel approach may open new avenues in selective cancer chemotherapy.

Selected as HOT, read this article for free now.

A self-immolative dendritic glucuronide prodrug of doxorubicin
Marion Grinda, Jonathan Clarhaut, Brigitte Renoux, Isabelle Tranoy-Opalinski and Sébastien Papot
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00193K, Concise Article

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Hot Perspective: Reviewing current knowledge on DNA methylation aspects

31 Oct 2011

In this MedChemComm article*, Nadine Martinet and colleagues at the Universities of Nice-Sophia Antipolis and Poitiers (France) provide a timely overview of the current knowledge concerning DNA methyltransferases (DNMT) biology and the two main classes of DNMT inhibtors, also highlighting epigenetic anti-cancer therapeutic strategies.

Read the article for FREE for the next 4 weeks!

Small molecules DNA methyltransferases inhibitors
Nadine Martinet, Benoît Y. Michel, Philippe Bertrand and Rachid Benhida
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00194A, Review

*This article will be part of MedChemComm’s web theme issue on Epigenetics, coming soon.

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Poster prize winner at the 16th SCI/RSC Medicinal Chemistry Symposium

12 Oct 2011

I am delighted to report that Dr Martine Keenan from Epichem Pty Ltd (Murdoch, Australia) was the winner of the MedChemComm poster prize at the recent 16th SCI/RSC Medicinal Chemistry Symposium that took place at Churchill College in Cambridge, UK, from 11 to 14 September.

The symposium was jointly organised by the Society of Chemical Industry and the Royal Society of Chemistry, and gave a splendid overview of some of the new strategies in Medicinal Chemistry and Pharmaceutical Research.

Martine’s winning poster entitled ‘Collaborative drug discovery for neglected diseases: novel compounds for the treatment of Chagas Disease’ presents the identification and development of two novel compound series active against the intracellular protozoan parasite Trypanosoma cruzi, the causative agent of the Chagas disease. Endemic in 21 countries across Latin America, the Chagas disease is responsible for more deaths in this region than Malaria, or any other parasite-born disease, and is currently spreading to developed countries including Australia, USA, Japan or Spain. This award winning work is the result of a collaborative drug discovery consortium established by not-for-profit, drug research and development organisation Drugs for Neglected Diseases initiative (DNDi).

Congratulations again to Martine on her award-winning work and to the collaborative drug delivery consortium for their active research on neglected diseases.

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Highly selective agonist for the metabotropic glutamate receptor mGluR2

05 Oct 2011

Work from this international collaboration spanning Denmark, Italy, Sweden and the USA brings insights into the synthesis and characterization of a selective agonist for the metabotropic glutamate receptor mGluR2, a potential therapeutic target for neurologic and psychiatric diseases.

The team’s approach to the agonist design was to induce selectivity for mGluR2 over other family members via imposing conformational rigidity into the carbon skeleton of the Glu analogues. This resulted in an increase of selectivity of at least two orders of magnitude compared to homologous mGluR3 as well as mGluR1, 4, 5, 7.

A highly selective agonist for the metabotropic glutamate receptor mGluR2
Simon D. Nielsen, Marica Fulco, Michaela Serpi, Birgitte Nielsen, Maria B. Hansen, Kasper L. Hansen, Christian Thomsen, Robb Brodbeck, Hans Bräuner-Osborne, Roberto Pellicciari, Per-Ola Norrby, Jeremy R. Greenwood and Rasmus P. Clausen

Interested? Why not read this MedChemComm article now! All our content is currently FREE to access .

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Biocompatible nanovalves as smart therapeutics for cancer therapy – A Review

09 Sep 2011

Biocompatible nanovalves can effectively store and protect drugs inside nano-reservoirs, then deliver and release them to kill targeted cancer cells under external stimuli. As such they are a promising example of smart materials that are devised to both address the controlled release of the therapeutics and selectively target diseased cells.

In this recent MedChemComm review article, Ying Wei Yang from Jilin University, Changchun (P.R China) provides a timely and comprehensive update on the recent progress of biocompatible nanovales based on mesoporous silica nanoparticles. The review highlights the cutting-edge progress in this field, with details of the nanovalves construction, therapeutic release mechanisms, while specifically focusing on the water-based systems for therapeutic applications.

Whether you are in the Medical, Materials or Chemistry field, this MedChemComm review is for you!

Free to access for the next 4 weeks.

Towards biocompatible nanovalves based on mesoporous silica nanoparticles Ying-Wei Yang
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00158B, Review

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Tubulin polymerization inhibitors on the cover of Issue 9

01 Sep 2011

Welcome to MedChemComm Issue 9.

Ahmed Kamal and colleagues from the Indian Institute of Chemical Technology in Hyderabad (India) have devised a series of novel 2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives through simple synthetic schemes that exhibit potent anticancer efficacy via the inhibition of tubulin polymerisation, thus blocking mitotic division.

Interested? Why not read the article now! As with all our Cover articles, it will be FREE to access for the next 6 weeks.

2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization Ahmed Kamal, Y. V. V. Srikanth, Thokhir B. Shaik, M. Naseer A. Khan, Md. Ashraf, M. Kashi Reddy, K. Anil Kumar and Shasi V. Kalivendi
Med. Chem. Commun., 2011, 2, 819-823 DOI: 10.1039/C0MD00177E

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RSC Medicinal Chemistry Blog

Author Archive

Epigenetics: a highly promising source of new drug targets

HOT Review: Epigenetic modulators for cancer chemotherapy

HOT: A self-immolative strategy to enhance cancer chemotherapy selectivity

Hot Perspective: Reviewing current knowledge on DNA methylation aspects

Poster prize winner at the 16th SCI/RSC Medicinal Chemistry Symposium

Highly selective agonist for the metabotropic glutamate receptor mGluR2

Biocompatible nanovalves as smart therapeutics for cancer therapy – A Review

Tubulin polymerization inhibitors on the cover of Issue 9

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