RSC Medicinal Chemistry Blog

Review: Gd(III) chelates for MRI contrast agents

02 Apr 2012

Kai-Hsiang Chuang and Chang-Tong Yang from the Singapore Bioimaging Consortium, A*STAR provide a timely review on the major developments of Gd(III) chelates as MRI contrast agents, from high relaxivity to ‘‘smart’’, from blood pool to blood–brain barrier.

The review covers:

Relaxivity of Gd(III) based MRI contrast agents
Smart contrast agents (pH-, metal ion-, enzyme- ; small biomolecule-activated)
Blood pool contrast agents (non-covalent binding to plasma proteins, polymeric and dendrimeric contrast agents)
Blood–brain barrier permeable contrast agents

Should your interests lie in coordination chemistry, polymer and supramolecular chemistry, medicinal chemistry, spectroscopy, biology or radiology, this review is for you!

Gd(III) chelates for MRI contrast agents: from high relaxivity to “smart”, from blood pool to blood–brain barrier permeable
Chang-Tong Yang and Kai-Hsiang Chuang
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C2MD00279E, Review Article

Why not also view our 2011 collection of topical review articles, across the full range of the journal scope, here.

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Computational screening of protein kinases on the cover of MedChemComm issue 4

28 Mar 2012

By James Anson.

The cover of this month’s issue of MedChemComm features work from Bonnet et al. on discriminating Type II kinase inhibitors from a large number of Type I and other decoy ligands taken from the MOE kinase and DUD databases. Have a read, it’s FREE to access for 6 weeks.

Targeting the inactive conformation of protein kinases: computational screening based on ligand conformation
Pascal Bonnet, Daniel Mucs and Richard A. Bryce
DOI: 10.1039/C1MD00256B

This issue also contains three reviews which you may find interesting:

Understanding and overcoming aminoglycoside resistance caused by N-6′-acetyltransferase
Kenward Vong and Karine Auclair
DOI: 10.1039/C2MD00253A

β-Lactams and β-lactones as activity-based probes in chemical biology
Thomas Böttcher and Stephan A. Sieber
DOI: 10.1039/C2MD00275B

The MEP pathway and the development of inhibitors as potential anti-infective agents
Ian Hale, Paul M. O’Neill, Neil G. Berry, Audrey Odom and Raman Sharma
DOI: 10.1039/C2MD00298A

View all this and much more HERE!

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Review of the biosynthetic MEP pathway and potential anti-infective agents

13 Mar 2012

By James Anson.

Audrey Odom, Raman Sharma and colleagues present a review examining the enzymes in the biosynthetic non-mevalonate (MEP) pathway from a detailed medicinal chemistry and structural biology perspective. The MEP pathway is utilised by plants but is absent in mammalian systems, making it a very attractive target for the development of potential next generation antimicrobial chemotherapeutics as well as novel herbicides.

Want to find out more about this pathway and its potential agents? You’re just a click away….

The MEP pathway and the development of inhibitors as potential anti-infective agents
Ian Hale, Paul M. O’Neill, Neil G. Berry, Audrey Odom and Raman Sharma
Med. Chem. Commun., DOI: 10.1039/C2MD00298A

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Review article on small-molecule inhibitors of dimeric transcription factors: a challenging area

13 Mar 2012

By James Anson.

Disruption of protein–protein or protein–DNA interactions involved in transcriptional machinery using small molecules poses a real challenge owing to several factors, including: the large interfacial areas involved, the lack of obvious binding sites, and the large free energy of association between the interfaces.

However, in recent years there has been considerable success in the dimeric transcription factor disruption using small molecules. Steven Fletcher and co-workers at University of Maryland School of Pharmacy, provide a review of the progress made in this area since 2008.

This review covers:

Inhibitors of STAT3
Inhibitors of c-Myc
Inhibitors of AP-1
Inhibitors of HIF-1

Small-molecule inhibitors of dimeric transcription factors: Antagonism of protein–protein and protein–DNA interactions
Jeremy L. Yap, Jay Chauhan, Kwan-Young Jung, Lijia Chen, Edward V. Prochownik and Steven Fletcher
Med. Chem. Commun., 2012,
DOI: 10.1039/C2MD00289B, Review

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Reviews on DNA methyltransferases, amphotericin B and antimalarial peroxides in Issue 3

06 Mar 2012

By Francesca Burgoyne.

On the cover of this month’s issue is an image from Nadine Martinet et al. accompanying their review on small molecule inhibitors of DNA methyltransferases. This article forms part of our recent Epigenetics collection, which also includes articles from Manfred Jung, Wolfgang Sippl, Antonello Mai and Stephen Frye.

Small molecules DNA methyltransferases inhibitors
Nadine Martinet, Benoît Y. Michel, Philippe Bertrand and Rachid Benhida
DOI: 10.1039/C1MD00194A

The issue also contains reviews from Peter Kovacic and Andrew Cooksy discussing the mechanism of the antifungal drug amphotericin B and Gary H. Posner et al. on recent advances in the design of cyclic peroxides for the treatment of malaria.

Novel, unifying mechanism for amphotericin B and other polyene drugs: electron affinity, radicals, electron transfer, autoxidation, toxicity, and antifungal action
Peter Kovacic and Andrew Cooksy
DOI: 10.1039/C2MD00267A

Antimalarial peroxides: advances in drug discovery and design
Rachel D. Slack, Alexander M. Jacobine and Gary H. Posner
DOI: 10.1039/C2MD00277A

View these and many other interesting articles online here

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Nominations now open – MedChemComm Emerging Investigator Lectureship

01 Mar 2012

By Richard Kelly.

Nominations are now open for the 2012 MedChemComm Emerging Investigator Lectureship. This new, annual Lectureship is given to recognise an emerging scientist who has made a significant contribution to their research field.

Members of the community are welcome to make a nomination for the Lectureship. In order to make a nomination, please contact the MedChemComm Editorial Office with the name and affiliation of the nominee and a brief description of why they should be considered. In order to be eligible for the MedChemComm Emerging Investigator Lectureship, the candidate should have completed their PhD on or after 31^st December 2001.

Nominations close on 31^st March 2012

The recipient of the Lectureship will be asked to present a lecture at an international meeting. The MedChemComm Editorial Office will provide a contribution to the recipient for travel and accommodation costs. The recipient of the Lectureship will be selected by a panel comprised of MedChemComm Editorial Board members.

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Review article on β-lactams and β-lactone probes for chemical biology

28 Feb 2012

By Francesca Burgoyne.

β-lactams and β-lactone probes for chemical biology Thomas Böttcher and Stephan A. Sieber here review the use of β-lactams and β-lactones for activity-based protein profiling. ABPP uses small molecules to target the active site of specific enzymes and is useful for understanding protein targets of natural products, drugs or synthetic libraries. β-Lactams and β-lactones are ideal probes for ABPP due to their so-called ‘privileged structures’, i.e. they have a core scaffold that can be recognised by a wide range of enzyme classes and can be ‘fine-tuned to obtain customized target selectivity’.

Take a look at this detailed review, which provides an update to of the field of activity-based β-lactam and β-lactone probes and their applications in chemical biology:

β-Lactams and β-lactones as activity-based probes in chemical biology
Thomas Böttcher and Stephan A. Sieber
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C2MD00275B

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RSC Medicinal Chemistry Blog

Review: Gd(III) chelates for MRI contrast agents

Computational screening of protein kinases on the cover of MedChemComm issue 4

Top ten most accessed articles in February

Review of the biosynthetic MEP pathway and potential anti-infective agents

Review article on small-molecule inhibitors of dimeric transcription factors: a challenging area

Top ten most accessed articles in January

Reviews on DNA methyltransferases, amphotericin B and antimalarial peroxides in Issue 3

Nominations now open – MedChemComm Emerging Investigator Lectureship

Review article on β-lactams and β-lactone probes for chemical biology

Top ten most accessed articles in December

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