Archive for the ‘Cover articles’ Category

Methanocarba ring as a ribose modification in ligands of G protein-coupled receptors on the cover of MedChemComm, Issue 4

Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors

Welcome to MedChemComm Issue 4, 2013!

Featuring on this month MedChemComm front cover is the work of Dilip K. Tosh and Kenneth A. Jacobson at the NIH in Bethesda, US:

Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches
Dilip K. Tosh and Kenneth A. Jacobson
DOI: 10.1039/c2md20348k

Free to access for 6 weeks 

This work had recenlty been highlighted on our blogs – why not read the full post here!

Also in this issue, read the review article on Metabolism-guided drug design by Amit S. Kalgutkar et al. at Pfizer Worldwide Research and Development, and much more!

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Issue 2 of MedChemComm featuring trehalose derivatives as potential therapeutic agents for Huntington’s disease

Welcome to this blog taking a look between the covers of this month’s issue of MedChemComm.

Preparation and evaluation of blood-brain barrier-permeable trehalose derivatives as potential therapeutic agents for Huntington's diseaseThis impressive image featuring on the front cover of the issue highlights the work being done by Kyong-Tai Kim and Sung-Kee Chung et al. Kim, Chung et al. have found a blood–brain barrier permeable derivative of trehalose that can prevent the aggregation of polyQ in transfected cells. This derivative was also found to prolong the lifespan and improve motor functions in a transgenic mouse model.

Preparation and evaluation of BBB-permeable trehalose derivatives as potential therapeutic agents for Huntington’s disease
Jungkyun Im, Sangjune Kim, Young-Hun Jeong, Wanil Kim, Dohyun Lee, Woo Sirl Lee, Young-Tae Chang, Kyong-Tai Kim and Sung-Kee Chung
DOI: 10.1039/C2MD20112G

Read the whole article for free for 6 weeks!


Also in this is issue:

Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B
Benjamin H. Fraser, K. Barry Sharpless et al.

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Themed Issue Highlighting New Talent In Medicinal Chemistry Now Published

Welcome to the first issue of MedChemComm of 2013. Join us in taking a look at our successes from the last year and in looking forward to another exciting year for the journal by reading our New Year Editorial.

Not only is this issue the first of a new year it is also our New Talent themed issue, where we showcase the strength of research being carried out by some of tomorrow’s leaders in the field with 36 high quality articles.

This stunning cover (right) highlights the work of Seung Bum Park et al. who have discovered a novel heterobiaryl pyrazolopyridine skeleton as a selective FLT3 inhibitor from phenotype-based viability profiling and hypothesis-driven deconvolution.

Discovery of a highly selective FLT3 kinase inhibitor from phenotypic cell viability profiling
Sanghee Lee, Ala Jo and Seung Bum Park
DOI: 10.1039/C2MD20169K

Stars, stars everywhere, and it’s not just the rising stars featured in this issue that we’re talking about with this cover (left) from Stephen P. Andrews and Benjamin Tehan. Andrews & Tehan review the first example of structure-based drug design with G protein-coupled receptors (GPCRs) thanks to StaR® proteins (stabilised GPCRs), and how this has enabled the identification of a preclinical candidate for the treatment of Parkinson’s disease.

Stabilised G protein-coupled receptors in structure-based drug design: a case study with adenosine A2A receptor

Stephen P. Andrews and Benjamin Tehan
DOI: 10.1039/C2MD20164J

Read it all today by visiting our journal home page.

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MedChemComm issue 12: featuring macrocyclization efficiency & transdermal insulin delivery

Welcome to issue 12 of MedChemComm, the last of 2012. This month we have 10 concise articles and 1 review for you to devour.

On the front cover:

Is this review from our collection on ‘The space in-between small molecules and biologicals’ by James C. Collins and Keith James. Collins and James present a critical analysis of macrocyclization reactions published over the past three years, and based on this propose a ‘macrocyclization efficiency index, Emac,’ which would allow the community to determine the true efficiency of a macrocyclization reaction.

Emac – a comparative index for the assessment of macrocyclization efficiency
James C. Collins and Keith James
DOI: 10.1039/C2MD20176C

On the inside cover:

Is this concise article from Masahiro Goto and colleagues who present their investigations into developing a unique, through the skin, protein-delivery system based on a solid-in-oil nanodispersion that utilizes an oil-based vehicle of proteins.

Transdermal delivery of insulin using a solid-in-oil nanodispersion enhanced by arginine-rich peptides
Yoshiro Tahara, Shota Honda, Noriho Kamiya and Masahiro Goto
DOI: 10.1039/C2MD20059G

Remember both of these articles are free to access for the next 6 weeks!

Get your hands on the last issue of 2012 today.

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TamiGold and tubulin polymerization inhibitors on MedChemComm’s covers this month

Wecome to MedChemComm Issue 11, 2012

Featuring on the front cover of this issue of MedChemComm is the work of Hansjörg Streicher and colleagues who report the strong and selective binding of 2 types of gold nanoparticles, decorated with the oseltamivir (aka TamifluTM) pharmacophore, to wild-type and resistant influenza virus strains. Streicher et al. describe how the particles interact with the virus neuraminidase rather than the hemagglutinin and could serve as a vantage point for novel influenza virus sensors.

‘TamiGold’: phospha-oseltamivir-stabilised gold nanoparticles as the basis for influenza therapeutics and diagnostics targeting the neuraminidase (instead of the hemagglutinin)
Mathew Stanley, Nicholas Cattle, John McCauley, Stephen R. Martin, Abdul Rashid, Robert A. Field, Benoit Carbain and Hansjörg Streicher
DOI: 10.1039/C2MD20034A

The inside front cover illustrates work by Ahmed Kamal et al. (CSIR-Indian Institute of Chemical Technology, Hyderabad), who have synthesized a new series of tetrazole based isoxazolines that show promising activity as tubulin polymerization inhibitors that could be developed for the treatment of cancer.

Synthesis of tetrazole–isoxazoline hybrids as a new class of tubulin polymerization inhibitors
Ahmed Kamal, A. Viswanath, M. Janaki Ramaiah, J. N. S. R. C. Murty, Farheen Sultana, G. Ramakrishna, Jaki R. Tamboli, S. N. C. V. L. Pushpavalli, Dhananjaya pal, Chandan Kishor, Anthony Addlagatta and Manika pal Bhadra
DOI: 10.1039/C2MD20085F

Enjoy FREE access to both articles for the next 6 weeks

Also in this issue, why not read  the following 2 review articles:

Small molecules targeting phosphoinositide 3-kinases
Peng Wu and Yongzhou Hu
Med. Chem. Commun., 2012, 3, 1337-1355
DOI: 10.1039/C2MD20044A

Diaryl ether derivatives as anticancer agents – a review
Florence Bedos-Belval, Anne Rouch, Corinne Vanucci-Bacqué and Michel Baltas
Med. Chem. Commun., 2012, 3, 1356-1372
DOI: 10.1039/C2MD20199B

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MedChemComm issue 10 now available online

The interesting image on the front cover of this month’s issue of MedChemComm is courtesy of Neil Vasdev and colleagues. Vasdev et al. present work which is aimed at developing a PET radiotracer based on a hydroxyquinoline chelator, and evaluates its potential for detecting amyloid plaques via imaging studies in transgenic rodent models.

Synthesis and PET imaging studies of [18F]2-fluoroquinolin-8-ol ([18F]CABS13) in transgenic mouse models of Alzheimer’s disease

Neil Vasdev et al.
DOI: 10.1039/C2MD20075A

The inside cover highlights the HOT article of Andreea R. Schmitzer and co-workers who report the factors intrinsic to imidazolium salts that are responsible for the salts’ ionophoric activity, allowing them to act as synthetic ion transporters.

An anion structure–activity relationship of imidazolium-based synthetic transporters
Claude-Rosny Elie, Mathieu Charbonneau and Andreea R. Schmitzer
DOI: 10.1039/C2MD20107K


Download both articles for free for the next 6 weeks.




Also in this issue is this HOT article from James S. Scott:

Reduction of acyl glucuronidation in a series of acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors: the discovery of AZD6925

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MedChemComm issue 9 now available

Issue 9 of MedChemComm has arrived….read it today!

Front cover:

Oral delivery of drugs aims to open up new areas of peptide/protein therapeutics associated with the removal for a need for injections. The major problems facing oral delivery of peptides/proteins is hydrolysis/proteolysis in the gastrointestinal tract and an inefficient uptake mechanism for peptides/proteins from the tract. Robert P. Doyle et al. are interested in the use of the vitamin B12 dietary uptake pathway to address these hurdles. In this paper Doyle et al. report the synthesis, purification and characterisation of a new B12-insulin conjugate attached between the B12 ribose hydroxyl group and insulin PheB1

Examining the effects of vitamin B12 conjugation on the biological activity of insulin: a molecular dynamic and in vivo oral uptake investigation
Susan Clardy-James, Damian G. Allis, Timothy J. Fairchild and Robert P. Doyle

Inside cover:

Doxorubicin (DOX) is a widely adopted chemotherapy treatment for many different varieties of cancer, but its clinical value is limited due to its systemic toxicity. Currently one of the best ways to minimize the dose-related toxic shortcoming of DOX is to encapsulate the drug in various drug-delivery systems. In this paper from Shiqi Peng and co-workers design a novel self-complexation and complexation controlled target drug carrier for DOX delivery.

Self-complexation and complexation-controlled target cancer therapy
Li Li, Ming Zhao, Wenhao Li, Yuji Wang, Zhuge Zhang, Ran An and Shiqi Peng

Also in this issue:

A review from James C. Knight and Frank R. Wuest, from University of Alberta, that aims to provide a comprehensive overview of the application of CXCR4-targeted imaging probes across both nuclear (positron emission tomography/single-photon emission computed tomography) and optical modalities.

Nuclear (PET/SPECT) and optical imaging probes targeting the CXCR4 chemokine receptor

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MedChemComm’s Natural Products themed issue now published online

Issue 8 of MedChemComm has arrived and it’s a Natural Products themed issue that is filled to bursting with: nine reviews elegantly summarising the synthesis, biosynthesis, inhibitory properties and targets, and biological functions of natural products, as well as new bioinformatics methods for their identification; and fourteen concise articles describing some of the newest discoveries in the field of natural products.


An example of such a concise article is featured on the inside cover of the issue:

Synthesis and anti-Helicobacter pylori activity of analogues of spirolaxine methyl ether
Ivaylo Dimitrov, Daniel P. Furkert, John D. Fraser, Fiona J. Radcliff, Orla Finch and Margaret A. Brimble
DOI: 10.1039/C2MD00314G

To check out the entire themed issue now click here…


A big thank you must go to the guest editors Professor Christopher Walsh (Harvard University) & Dr Sylvie Garneau-Tsodikova (University of Michigan) for all their hard work, and to all those who have contributed to this issue for making this issue such a success.

Finally, below is a cover suggestion from Amanda J. Hughes et al., which we really liked but which we were unfortunately unable to use on the cover, so we thought we would share it with you here.

Employing a polyketide synthase module and thioesterase in the semipreparative biocatalysis of diverse triketide pyrones
Amanda J. Hughes, Joshua F. Detelich and Adrian T. Keatinge-Clay
DOI: 10.1039/C2MD20013A

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Get your hands on MedChemComm issue 7 today!

This striking cover brings the work of Patrick T. Gunning and co-workers to the forefront of issue 7.

In this Concise article Gunning et al. discuss the design and synthesis of a novel class of ditopic coordination complex-based SH2 domain mimetics using de novo rational and computational design. In addition Gunning et al. identify several lead compounds that bind selectively to target phosphopeptides via the same bivalent binding mechanism employed by SH2 domains in a cell.

Access this article for FREE for 6 weeks!

Src homology 2 domain proteomimetics: developing phosphopeptide selective receptors
Joel A. Drewry, Steven Burger, Amir Mazouchi, Eugenia Duodu, Paul Ayers, Claudiu C. Gradinaru and Patrick T. Gunning

Also in this issue are the following 2 reviews:

The use of phosphate bioisosteres in medicinal chemistry and chemical biology
Thomas S. Elliott, Aine Slowey, Yulin Ye and Stuart J. Conway

M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer’s disease
Michael Decker and Ulrike Holzgrabe

Check out all this and more in the complete online issue

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MedChemComm issue 6 published online

The front cover of this issue of MedChemComm highlights the work of Philip J. Johnson, Mikhail Y. Berezin and colleagues. As part of the long term goal of developing nerve specific near infrared (NIR) molecular probes capable of non-invasively assessing peripheral nerve damage, in this concise article Berezin et al. present a study on the identification of a NIR dye suitable for such probes, focusing on a novel highly hydrophilic and functionalisable polymethine dye, and its more hydrophobic analogue indocyanine green.

A NIR dye for development of peripheral nerve targeted probes
Tiffany P. Gustafson,  Ying Yan,  Piyaraj Newton,  Daniel A. Hunter,  Samuel Achilefu,  Walter J. Akers,  Susan E. Mackinnon,  Philip J. Johnson and Mikhail Y. Berezin
DOI: 10.1039/C2MD00297C

Also in this issue is the review by Georges Vauquelin on:
Determination of drug–receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance
DOI: 10.1039/C2MD20015E

View the entire issue here….

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