MedChemComm is delighted to announce a high-profile themed issue on Phenotypic Drug Discovery,due for publication online in mid-2016. The issue is being Guest Edited by Dr Fabien Vincent (Pfizer), Dr Jonathan A. Lee (Eli Lilly) and Professor Michael Pollastri (Northeastern University).
Deadline for Submission: February 1, 2016
The level of quality of this issue will be high, and all manuscripts will subject to the journal’s normal standards and peer review process. Guidelines are available at rsc.li/1K0EgYx and rsc.li/1JAwCbA
If you are interested in taking part in this issue, please email MedChemComm: medchemcomm-rsc@rsc.org
Scope of the issue
Phenotypic approaches are highly complementary to the molecular target centric strategy that prevails in Pharma and moreover, may mitigate future clinical failure issues related to target validation and lack of efficacy. Five years into the Phenotypic Drug Discovery (PDD) Renaissance, this issue aims to shift the main focus in this area from assays and screens towards the medicinal chemistry programs engendered by these early efforts. Manuscripts covering the lessons learned and progress recorded on the road to clinical candidates in the areas highlighted below are actively sought:
Design of compound libraries for phenotypic screening (e.g. biologically annotated, diversity-based and natural products libraries)
Identification of novel targets for disease-relevant phenotypes
Identification of novel chemical matter or molecular mechanisms of action for known molecular targets
Identification of novel cellular roles for known targets
Challenges in PDD hit triage such as compound/series prioritization and validation
Challenges in driving an SAR using complex assay systems (in vitro and in vivo systems)
Safety derisking and compound/project progression in the absence of a known target
Chemical biology approaches for mechanism and target deconvolution
New research in MedChemComm is published as Concise Articles. This article type encompasses both Communication and Full Paper styles with no strict page limit. There is also the opportunity to write a Review article for the issue, and if you would be interested in this please let us know.
MedChemComm is the Royal Society of Chemistry journal covering all areas of medicinal chemistry research, including research that interfaces with other areas of the chemical sciences, biology, materials science or physics
The journal is in partnership with the European Federation for Medicinal Chemistry (EFMC), and the co-Editors-in-Chief are Dr. Tony Wood (Pfizer) and Professor Greg Verdine (Harvard University). To view recent articles or to find out more about the journal please visit the website at www.rsc.org/medchemcomm
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MedChemComm is delighted to announce a high-profile themed issue on Membrane Transporters, focussing on solute carriers (SLCs). The Guest Editors for this issue are Professor Matthias A. Hediger (University of Bern, Switzerland) and Dr David Hepworth (Pfizer, Cambridge, USA).
Manuscripts can be submitted using the Royal Society of Chemistry’s online article submission service. Please clearly state that the manuscript is submitted for the themed issue on Membrane Transporters: Solute Carriers.
The level of quality of this issue will be high, and all manuscripts will undergo the journal’s normal peer review process.
Scope
Metabolic homeostasis within cells requires strict control over the import and export of metabolites, nutrients and ions across membranes. Polar chemical species such as these have negligible ability to cross phospholipid membranes by simple diffusion and instead require highly regulated transport proteins to control their movement. The largest class of transport proteins is the solute carrier series (www.bioparadigms.org) and it is on this superfamily that this special issue of MedChemComm will focus.
These proteins are of great interest for basic academic research, but beyond that they are of central importance in a number of areas of applied science: as drug targets, as controllers of drug disposition and pharmacokinetics, and as the cause of drug toxicity.
Known SLC drug targets include:
The monoamine transporter family which contains the serotonin transporter (SLC6A4) target of the highly important SSRI drug class
SLC5A2 (SGLT2), an important new anti-diabetic target to block renal glucose reabsorption
Sodium chloride transporters (SLC12 family) – the targets of loop and thiazide diuretics
SLCs important in drug pharmacokinetics and disposition include
The OATP (SLCO) and OAT (SLC22) family of anion transport
The OCT (SLC22) family of cation transport
The SLC47 multidrug and toxin extrusion family
SLCs important in drug toxicity include the thiamine transporter SLC19A2
All areas of research where the chemical sciences have impacted the study of the SLC superfamily will be considered for inclusion in this themed issue. Examples include, but are not limited to:
Medicinal chemistry and molecular probe design against these target families
Chemical biology approaches to allow for detailed study of these protein classes including physiological roles, disease mechanisms, etc.
Structural biology and biophysics of integral membrane proteins as relevant to ligand design and/or chemical biology
Molecular modelling that has enabled drug and probe design
The impact of transporters on drug disposition and pharmacokinetics – with a particular interest in structure activity relationships for such transport
The study of toxins and venoms which act through these target classes
Novel screening methodologies that allow the identification of new inhibitors, modulators and substrates of this protein class
The application of new cell biology techniques such as gene-editing, silencing and haploid genetic approaches that allow the study of chemical agents acting via these target families
Systems biology approaches to the study of chemical modulators and substrates of membrane transport proteins
The issue will consist of a series of research articles and reviews from prominent scientists who are committed to applying excellence in ion channels and membrane transporter research toward the treatment of human diseases, combining breakthroughs in both basic science and applied science, such as drug discovery.
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Professor Richard Payne to present his lecturre at Chemical Protein Synthesis Meeting
Earlier this year Professor Richard Payne from University of Sydney, Australia, was announced as the the recipient of the 2015 MedChemComm Emerging Investigator Lectureship.
We are pleased to let you know that Richard will be presenting his talk entilted:
‘New ligation technologies for the rapid assembly of modified proteins‘
The meeting starts on the 16th of June 2015 and online registration for the meeting closes the 10th of June – so there’s still time to register to see Richard’s talk!
UPDATE: Prof. Payne’s talk was very well received at the successful Chemical Protein Synthesis Meeting, where he (left) was presented his lectureship by Professor Stephen Kent (right).
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The Wellcome Trust is seeking 10 enthusiastic junior researchers currently undertaking interdisciplinary research, or who are wishing to pursue interdisciplinary collaborations, to attend their first Frontier meeting: One Science – Life at the Interface on 21-22 September 2015. Applications close on Friday 12th June 2015.
For full details, click on the image below
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We are delighted to share with you a collection of research papers, review articles and books on the topic of antimicrobial resistance (AMR). Warnings about the threat of antibiotic resistance, and more broadly AMR, to human health, global food production and economic prosperity are receiving increased media interest. By 2050, it is estimated that without coordinated action, 10 million people could die from previously curable illnesses.
“At the end of this month, the World Health Organisation (WHO) will present their draft global action plan on AMR at the 68th World Health Assembly in Geneva, it is timely to consider the importance of chemistry in tackling antimicrobial resistance,” comments Professor Sylvie Garneau-Tsodikova, Editorial Board member of MedChemComm “This collection showcases the essential contributions of chemical science to understanding antibiotic resistance, developing new treatments, diagnostics and mitigations strategies to tackle this global threat.”
“The chemical sciences play a pivotal role in a sustainable and prosperous future” says Dominic Tildesley, President of the Royal Society of Chemistry “whether it’s developing new antibiotics to combat infection, converting waste to energy, or developing efficient solar energy cells, chemists are designing and applying tomorrow’s technologies”.
All articles are freely available until 18th June. All books included here have their first chapter free to read.
Having trouble acessing the articles? Remeber to login in to you free personal account to see all our free content.
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Why is it important to address AMR?
Thomas Fleming outlines the role of chemistry in tackling antibiotic resistance as part of our recent chemistry in health video competition
Beating the Superbugs – avoiding an antibiotic apocalypse – a public panel discussion chaired by Michael Moseley, science journalist and TV presenter, with scientists and policy makers to discuss the challenges and possible solutions to addressing AMR.
Antibiotics from myxobacteria
Till F. Schäberle, Friederike Lohr, Alexander Schmitz and Gabriele M. König Nat. Prod. Rep., DOI: 10.1039/C4NP00011K, Review Article
AApeptides as a new class of antimicrobial agents
Youhong Niu, Haifan Wu, Yaqiong Li, Yaogang Hu, Shruti Padhee, Qi Li, Chuanhai Cao and Jianfeng Cai Org. Biomol. Chem., DOI: 10.1039/C3OB40444G, Perspective
Inhibitors of bacterial tubulin target bacterial membranes in vivo
Marie H. Foss, Ye-Jin Eun, Charles I. Grove, Daniel A. Pauw, Nohemy A. Sorto, Jarred W. Rensvold, David J. Pagliarini, Jared T. Shaw and Douglas B. Weibel Med. Chem. Commun., DOI: 10.1039/C2MD20127E, Concise Article
Dr Matthew Fuchter is a Senior Lecturer in Synthetic and Medicinal Chemistry within the Synthesis Group at the Department of Chemistry at Imperial College.
He completed PhD research under the supervision of Professor A. G. M. Barrett, FRS FMedSci and postdoctoral studies at the Commonwealth Scientific and Industrial Research Organisation, Australia, where he worked with Professor A. B. Holmes, FRS.
Prior to his position at Imperial College he was the RCUK Academic Fellow in Cancer Medicinal Chemistry at the School of Pharmacy (University of London). He returned to Imperial College in July 2008 as a Lecturer in Synthetic and Medicinal Chemistry and was promoted to Senior Lecturer in July 2012.
In 2014 he was awarded the RSC Harrison-Meldola Memorial Prize, as well as being admitted to the Royal Society of Chemistry as a Fellow.
At Imperial College he is heavily involved in research at the interface of chemistry and medicine. For example, he is a Managerial Board member of the anti-cancer drug discovery group, a Research Board member of the Institute of Chemical Biology and co-Director of the MRes in Drug Discovery.
The Medicinal Chemistry Toolkit App, compatible with iOS devices and optimised for iPad, provides a suite of resources to support the day to day work of a medicinal chemist.
Potency shift due to plasma protein binding calculator
LogD vs pH curves
Attrition modeller
Drug-drug interaction modeller
Exciting new functionalityrecently released in v2.0 allows you to draw your own structures and provides direct feedback on the quality or drug-like nature of your compound and calculates pharmacologically relevant properties (GClogP, ligand efficiency).
The app has been designed in collaboration with the editors of The Handbook of Medicinal Chemistry: Principles and Practice, which was published in December 2014 providing a comprehensive, everyday resource for a practicing medicinal chemist throughout the drug development process.
Comprehensive and up-to-date information covering the entire drug development process.
Written and edited by experts from academia and industry.
Case studies with hints and tips from within the industry allow medicinal chemists to apply academic understanding to drug discovery.
Coming Soon: interactive electronic format
The Handbook will be published online to allow greater linking to relevant resources. Per chapter download from our publication platform containing additional features, such as links to protein and chemical structures, interactive graphs and downloadable project management templates, will be available soon.
PDF eISBN: 978-1-78262-183-6
EPUB eISBN: 978-1-78262-419-6
DOI: 10.1039/9781782621836
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Andrea Cavalli is Professor of Medicinal Chemistry at the University of Bologna and Head of CompuNet at the Italian Istitute of Tecnology, Genova. Prof. Cavalli received his PhD in Pharmaceutical Sciences from the University of Bologna in 1999 and did postdoctoral work at SISSA (Trieste, Italy) and ETH (Zurich, Switzerland).
Prof. Cavalli’s research has combined computational chemistry with drug discovery, focusing on neurodegenerative diseases, cancer, and neglected tropical diseases. He has developed and applied computational tools and protocols to accelerate and enhance the discovery of novel lead and drug candidates. In particular, he has been a pioneer in the use of molecular dynamics simulations and related approaches to drug discovery. He is co-founder of a high-tech startup company (BiKi Technologies s.r.l.) focused on molecular dynamics and enhanced sampling in drug discovery. In an interdisciplinary effort, these approaches led to the identification and characterization of lead candidates within the framework of multitarget drug discovery and polypharmacology.
He is an author of more than 160 scientific articles published in high-ranked journals and inventor in several international patents. He has delivered numerous invited lectures and seminars at international congresses and prestigious institutions. In 2003, he was awarded the Farmindustria Prize for Pharmaceutical Research.
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Koen Augustyns obtained his Master and PhD in Pharmaceutical Sciences at the KU Leuven, Belgium in 1988 and 1992 respectively. After postdoctoral stays at the University of Antwerp, Belgium and the University of Tübingen, Germany he was appointed as Professor of Medicinal Chemistry at the University of Antwerp, Belgium.
His research has resulted in 135 papers (2727 citations, h-index 30) and 12 patents in the field of medicinal chemistry, mostly focused on the design and development of enzyme inhibitors in the fields of oncology and infectious diseases. Recently he has also been active in the field of activity-based probes and bioorthogonal chemistry. So far, he has supervised 20 PhD students and is currently heading an international research group of 25 PhD students and postdoctoral scientists. He has delivered over 30 invited lectures at international symposia and acted as promoter on over 60 research projects.
He was chair of the Department of Pharmaceutical Sciences from 2007-2012 and is currently vice-dean of the Faculty of Pharmaceutical, Biomedical and Veterinary Sciences at the University of Antwerp. Since 2002, he is the President of the Medicinal and Bioorganic Chemistry Division of the Royal Flemish Chemical Society (KVCV) in Belgium and he serves the European Federation for Medicinal Chemistry (EFMC) as Secretary (2009-2013), President-Elect (2014) and President (2015-2017). He is a member of the Commission on Innovation Policy of the Flemish Council for Science and Innovation, the Research Foundation Flanders and the Jury of the Prix Galien Belgium. He is and was a member of several international organizing committees of medicinal chemistry symposia, and was co-chair of the EFMC-International Symposium on Medicinal Chemistry in 2010 in Brussels.
Chemistry in Health 2015 – Towards new therapeutics to fight disease 26 May, Burlington House, London, UK
This free to attend symposium will focus on the development of new therapies to fight infectious diseases, in particular highlighting the important role of chemistry and biochemistry. Tackling antimicrobial resistance will require researchers from a range of disciplines to work together and this event will showcase leading research from a number of our recent Prize and Award winners.
Taking place during the same month that the World Health Organisation will present their draft global action plan on antimicrobial resistance at the World Health Assembly, this symposium presents a timely opportunity to highlight the role of science in mitigating antimicrobial resistance. We will also explore the development of new improved platforms for collaboration, such as Public Private Partnerships (PPP), which enable the research and development that is needed to better deliver the medicines of the future.
A poster session will be held over lunch. Poster abstract deadline: 29 April 2015.
For more information about the speaker line up and to register please visit the event page. Registration deadline: 8 May 2015.
Non-classical β-carbonic anhydrase inhibitors-towards novel anti-mycobacterials
Thiazole-based aminopyrimidines and N-phenylpyrazolines as potent antimicrobial agents: synthesis and biological evaluation
Silver in Healthcare: Its Antimicrobial Efficacy and Safety in Use
