Archive for the ‘Themed Issues’ Category

Epigenetics: a highly promising source of new drug targets

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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Drug-target residence times and covalent binders themed issue – call for papers

On behalf of Professor Dr Koen Augustyns (University of Antwerp), Guest Editor, we would like to invite authors to contribute to this themed issue which aims collect together in one place some of the latest exciting research from across the breadth of drug residence and covalent drug research.

Analysis of drug-target residence time has begun to play a larger role in drug discovery as suggested by recent literature. For compounds with a slow off rate, long action at the target may render a perfect pharmacokinetic profile unnecessary, and selectivity vs. other targets inhibited only briefly may be more readily achieved. Reversible and irreversible covalent binding drugs may be considered as the logical extreme for this approach. For other targets or therapeutic areas, other kinetic profiles may be desirable. Finally, there is a real need to build a better understanding in the medicinal chemistry community of the preferred profiles, screening methods, at which stage of a project lifetime to characterize the kinetics, and ideally a structural bases for design to achieve a desired kinetic profile.

-Koen Augustyns, Guest Editor

Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work. In addition, as this is a web-based theme issue, printing of articles will not be held for a specific issue thereby allowing rapid dissemination of the science presented online and in print without delay. Both reviews and primary research are suitable for this issue.

The submission deadline for the web theme issue will be Monday 6th February 2012.

If you would like to contribute to this exciting themed issue, please contact the Editorial Office.

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Themed issue on Drug-Target Residence Times – deadline extended

We are pleased to inform our authors that we will be extending the submission deadline for our forthcoming drug-target residence times web theme issue to Monday 6th February 2012.

The issue will be guest edited by Professor Dr Koen Augustyns (University of Antwerp) and aims collect together in one place some of the latest exciting research from across the breadth of drug residence research.

Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work. In addition, as this is a web-based theme issue, printing of articles will not be held for a specific issue thereby allowing rapid dissemination of the science presented online and in print without delay. Both reviews and primary research are suitable for this issue.

If you would like to contribute to this exciting themed issue, please contact the Editorial Office.

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HOT: Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy

This review from Manfred Jung and colleagues looks at the structural biology and inhibition of bromodomains, enzymatic domains which recognise acetylated lysines residues in modified histones in chromatin.  Inhibiting the protein–protein interactions in bromodomains by using small molecules as epigenetic tools is an exciting new area of research, offering potential for new therapeutic approaches.

The review includes:

  • Structural features of bromodomains and acetyl-lysine recognition
  • Implication of bromodomains in pathological cellular states
  • Challenges by targeting protein–protein interactions with small molecules
  • Inhibitors of bromodomain-mediated protein–protein interactions
  • Inhibitors of the PCAF-BRD/HIV-TatK50ac interaction
  • Inhibitors of the CBP-BRD/p53K382ac interaction
  • Inhibitors of BET bromodomains

This hot review is part of our forthcoming themed issue on Epigenetics – keep checking back for more hot research in this theme:

Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy
Silviya D. Furdas, Luca Carlino, Wolfgang Sippl and Manfred Jung
DOI: 10.1039/C1MD00201E

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Development of second generation epigenetic agents

This hot review from Philip Jones, MD Anderson Cancer Center, Texas, examines our understanding of the structure and function of epigenetic enzymes, including lysine and arginine methyltransferases and demethylases, histone acetyl transferases and histone deacetylases, and the chemical probes and tools available to increase our understanding.

It focuses on the development of a second generation of epigenetic agents able to manipulate histone modifications responsible for aberrant epigenetic gene transcription associated with disease states.

Areas covered:

  • Class I and II HDAC inhibitors
  • HDAC 1-4, 6, 8 selective inhibitors
  • Class III HDAC inhibitors
  • Histone acetyl transferase inhibitors
  • Histone methyltransferase inhibitors
  • Lysine and arginine methyltransferase inhibitors
  • Histone demethylase inhibitors
  • Lysine specific demethylase 1 inhibitors
  • JmJ demethylase inhibitors

Development of second generation epigenetic agents
Philip Jones
DOI: 10.1039/C1MD00199J

This article is part of our forthcoming themed issue on Epigenetics – check back soon for more hot articles in this issue!

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Hot Perspective: Reviewing current knowledge on DNA methylation aspects

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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Are pyridazines privileged structures?

Camille Wermuth, Prestwick Chemical Inc., France, presents an interesting account of the use, and potential, of pyridazine scaffolds in medicinal chemistry in this hot review.  He suggests that the pyridazine scaffold is a privileged structure, i.e. it is capable of providing useful ligands for more than one receptor, and has several advantages over the commonly used phenyl ring.

This article is part of the collection: 21st International Symposium on Medicinal Chemistry (EFMC-ISMC 2010) and is free to access:

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00074H

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Call for papers – MedChemComm Natural Products themed issue

We are delighted to announce a special themed issue of MedChemComm on Natural Products, due for publication in summer 2012

This themed issue, guest edited by Professor Christopher T. Walsh and Dr Sylvie Garneau-Tsodikova will collect together in one place some of the latest exciting research natural products chemistry, including, but not limited to: biosynthesis, novel natural products as drug or drug leads, novel technologies for natural products discovery, novel chemical transformations in natural product biosynthesis, as well as chemical and chemoenzymatic synthesis of natural products. Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work.

Deadline for Submission: January 31, 2012. Although publication of the issue is scheduled for summer 2012, web publication of the Advance Article versions of each manuscript will proceed as soon as the article is ready, ensuring that research is disseminated without delay.

Manuscripts can be submitted using the online web submissions service at http://mc.manuscriptcentral.com/mcc. Please indicate on submission in the comments to editor section that your manuscript is invited and intended for the Natural Products themed issue.

For more information please contact the Editorial Office.

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