Reviews – Page 5 – RSC Medicinal Chemistry Blog

Archive for the ‘Reviews’ Category

Tracking immune cell migration on the cover of Issue 11

04 Nov 2011

On the cover of Issue 11 is a hot article from Mark Bradley and coworkers on a method to track innate immune cell migration in vivo using dye-labelled peptoids.

Far red and NIR dye-peptoid conjugates for efficient immune cell labelling and tracking in preclinical models
Kevin Dhaliwal, Géraldine Escher, Asier Unciti-Broceta, Neil McDonald, A. John Simpson, Chris Haslett and Mark Bradley
Med. Chem. Commun., 2011, 2, 1050-1053
DOI: 10.1039/C1MD00171J

Also in this issue is Ying-Wei Yang’s review on biocompatible nanovalves for drug delivery and release:

Towards biocompatible nanovalves based on mesoporous silica nanoparticles
Ying-Wei Yang
Med. Chem. Commun., 2011, 2, 1033-1049
DOI: 10.1039/C1MD00158B

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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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Current progress in inhibiting Stat5 protein signalling

14 Oct 2011

This mini-review from Patrick Gunning et al. looks at progress made towards inhibiting Stat5, a member of the Stat family of signalling proteins, that is connected to many cancers, including acute myeloid leukemias and prostate cancer.

Areas covered include both direct and indirect inhibition:

Bcr/Abl inhibitors
FLT3 inhibitors
Jak2 inhibitors
truncation inhibitors
Binding to DNA
Disrupting dimerisation

Inhibitors of Stat5 protein signalling
Abbarna A. Cumaraswamy, Aleksandra Todic, Diana Resetca, Mark D. Minden and Patrick T. Gunning
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00175B

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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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Review: Practical use of Minisci reactions

09 Sep 2011

In this MedChemComm review Matthew Duncton, Renovis Inc., highlights the attractive potential of Minisci reactions – addition of radicals to heteroaromatic bases – for medicinal and biological chemists.

These reactions can be used to introduce a broad-range of selective CH-functionalization groups, such as alkyls, cycloalkyls, sugars, esters and more. In many cases, these processes are highly chemo- and regio-selective, making them ideal for industrial applications, because complicating factors such as protecting group strategies can be avoided.

Graphical abstract: Minisci reactions: Versatile CH-functionalizations for medicinal chemists

Read this review now for specific examples and future developments of these useful reactions. It’s free to download for the next 4 weeks!

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton, Med. Chem. Commun., 2011, DOI: 10.1039/C1MD00134E

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Progress on lamellarins

01 Aug 2011

This review article from Mercedes Álvarez and colleagues at The Center for Biomedical Research Network in Bioengineering, Biomaterials and Nanomedicine, Barcelona, have reviewed the recent developments in studies on lamellarins and their analogues.

Lamellarins are a family of marine pyrrole alkaloids, which have attracted interest as anti-tumour agents. The review encompasses synthetic strategies for total synthesis, structure–activity relationships and studies on mechanisms of biological action, mainly in the context of anti-tumor activity.

Download the full article here:

Progress on lamellarins
Daniel Pla, Fernando Albericio and Mercedes Álvarez
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00003A

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Are pyridazines privileged structures?

04 Jul 2011

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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Review: latest information on MDMX – the alternative regulator of p53

08 Jun 2011

The p53 signalling pathway is responsible for regulating the cell cycle, initiating DNA repair and triggering apoptosis where necessary. Its crucial importance can clearly be seen by the fact that about half of human cancers contain alterations in the p53 pathway. The proteins MDM2 and MDMX (a.k.a. MDM4) negatively regulate p53, and altered levels of these proteins are often deemed responsible for p53 alterations. As a result MDM2 has been extensively studied, but few MDM2 inhibitors have made it as far as clinical trials.

In this review Antonio Macchiarulo (University of Perugia) and team have sought to pull together recent breakthroughs on the lesser studied MDMX. MDMX is structurally similar to MDM2, but interestingly cells appear unable to compensate for the loss of one negative regulator with the other – they regulate non-overlapping functions. The review highlights new structural information available for MDMX and recent studies on the potential of dual MDMX and MDM2 inhibitors. The conclusion – we need to develop more small molecules selective for MDMX to further understand and validate its potential as a therapeutic target.

This interesting article is on the cover of our latest issue – Issue 6 – and is currently free to access:

Expanding the horizon of chemotherapeutic targets: From MDM2 to MDMX (MDM4)
Antonio Macchiarulo, Nicola Giacchè, Andrea Carotti, Fabiola Moretti and Roberto Pellicciari
Med. Chem. Commun., 2011, 2, 455-465
DOI: 10.1039/C0MD00238K

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HOT perspective: drug discovery – overweight and in need of a psychologist?

09 Mar 2011

In this interesting review Michael Hann from GSK gives his take on why it is becoming harder and harder to bring drugs to market. The finger of blame, he suggests, points not just towards regulatory hurdles but to our ideas about the drug discovery process itself.

As well as examining the causes of failure in drug discovery in terms of lead candidate properties, he also takes a look at the behavioural psychology of the medicinal chemist. Hann suggests that the quest for the potency borders on addiction, and that while potency is an important aspect of drug design, it should not necessarily be the overarching goal. His reason – that the search for potency can lead to molecules that are too large and liphophilic to make it to market. He ironically coins the term ‘molecular obesity‘ to describe the risk that this presents to the fitness of lead compounds.

Whether you agree with Hann on the cause of failure or not, the 95% attrition rate of pharma R&D is indisputable; it would appear that drug discovery is in need of a check-up.

Download this though-provoking review today – it’s free to access until April:

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00017A

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Extending the life of peptides

25 Oct 2010

Christian Heinis and Lisa Pollaro talk about different strategies to prolong the in vivo plasma residence time of peptides.

Several strategies that extend the elimination half-life of peptides from minutes to several hours or even days are described in this interesting review.

You can read it for free here

Strategies to prolong the plasma residence time of peptide drugs
Lisa Pollaro and Christian Heinis
Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00111B, Review

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