Author Archive

Phenotypic Drug Discovery Web Themed Issue

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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Membrane Transporters: Solute Carriers themed issue launched

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).

Deadline for Submission: December 14 2015

Please e-mail the Editorial Office if you are interested in contributing an article.

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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2015 Emerging Investigator Lectureship

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

at the upcoming Chemical Protein Synthesis (CPS) Meeting in St. Augustine, Florida on Friday the 19th of June.

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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Wellcome Trust Frontier meeting: One Science – Life at the Interface

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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Antimicrobial Resistance Article Collection

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.

© iStock

“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.

Learn more about our work to support the chemical sciences community working on solutions in climate change, energy, food, health and water.

Having trouble acessing the articles? Remeber to login in to you free personal account to see all our free content.
Don’t have a free account? It’s quick and easy to create one now.


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.

Design & synthesis of new antimicrobials


Reviews and Perspectives:

Plants as sources of new antimicrobials and resistance-modifying agents
Ana Cristina Abreu, Andrew J. McBain and Manuel Simões
Nat. Prod. Rep., DOI: 10.1039/C2NP20035J, Review Article

Antibiotics from myxobacteria
Till F. Schäberle, Friederike Lohr, Alexander Schmitz and Gabriele M. König
Nat. Prod. Rep., DOI: 10.1039/C4NP00011K, Review Article

Glycopeptide dendrimers as Pseudomonas aeruginosa biofilm inhibitors
Jean-Louis Reymond, Myriam Bergmann and Tamis Darbre
Chem. Soc. Rev., DOI: 10.1039/C3CS35504G, Review Article

Dithiolopyrrolones: biosynthesis, synthesis, and activity of a unique class of disulfide-containing antibiotics
Bo Li, Walter J. Wever, Christopher T. Walsh and Albert A. Bowers
Nat. Prod. Rep., DOI: 10.1039/C3NP70106A, Review Article

Ruthenium complexes as antimicrobial agents
Fangfei Li, J. Grant Collins and F. Richard Keene
Chem. Soc. Rev., DOI: 10.1039/C4CS00343H, 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

Benzyl-substituted metallocarbene antibiotics and anticancer drugs
F. Hackenberg and M. Tacke
Dalton Trans., DOI: 10.1039/C4DT00624K, Perspective

Siderophore-dependent iron uptake systems as gates for antibiotic Trojan horse strategies against Pseudomonas aeruginosa
Gaëtan L. A. Mislin and Isabelle J. Schalk
Metallomics, DOI: 10.1039/C3MT00359K, Minireview

Design and synthesis of membrane-targeting antibiotics: from peptides- to aminosugar-based antimicrobial cationic amphiphiles
Ido M. Herzog and Micha Fridman
Med. Chem. Commun., DOI: 10.1039/C4MD00012A, Review Article


Original research articles:

Synthesis of antimicrobial cyclodextrins bearing polyarylamino and polyalkylamino groups via click chemistry for bacterial membrane disruption
Hatsuo Yamamura, Yuuki Sugiyama, Kensuke Murata, Takanori Yokoi, Ryuji Kurata, Atsushi Miyagawa, Kenji Sakamoto, Keiko Komagoe, Tsuyoshi Inoue and Takashi Katsu
Chem. Commun., DOI: 10.1039/C3CC49543D, Communication

Phenazine antibiotic inspired discovery of potent bromophenazine antibacterial agents against Staphylococcus aureus and Staphylococcus epidermidis
Nicholas V. Borrero, Fang Bai, Cristian Perez, Benjamin Q. Duong, James R. Rocca, Shouguang Jin and Robert W. Huigens III
Org. Biomol. Chem., DOI: 10.1039/C3OB42416B, Communication

Polymers with tunable side-chain amphiphilicity as non-hemolytic antibacterial agents
Divakara S. S. M. Uppu, Padma Akkapeddi, Goutham B. Manjunath, Venkateswarlu Yarlagadda, Jiaul Hoque and Jayanta Haldar
Chem. Commun., DOI: 10.1039/C3CC43751E, Communication

Mechanism of Action of the Uridyl Peptide Antibiotics: An Unexpected Link to a Protein-Protein Interaction Site in Translocase MraY
Timothy Bugg, Maria Rodolis, Agnes Mihalyi, Christian Ducho, Kornelia Eitel, Bertolt Gust and Rebecca Jane Miriam Goss
Chem. Commun., DOI: 10.1039/C4CC06516F, Communication

Tailored lysozyme–ZnO nanoparticle conjugates as nanoantibiotics
Nirmalya Tripathy, Rafiq Ahmad, Seung Hyuck Bang, Jiho Min and Yoon-Bong Hahn
Chem. Commun., DOI: 10.1039/C4CC03712J, Communication

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

A structure activity-relationship study of the bacterial signal molecule HHQ reveals swarming motility inhibition in Bacillus atrophaeus
F. Jerry Reen, Rachel Shanahan, Rafael Cano, Fergal O’Gara and Gerard P. McGlacken
Org. Biomol. Chem., DOI: 10.1039/C5OB00315F, Paper

An organometallic structure-activity relationship study reveals the essential role of a Re(CO)3 moiety in the activity against gram-positive pathogens including MRSA
Malay Patra, Michaela Wenzel, Pascal Prochnow, Vanessa Pierroz, Gilles Gasser, Julia E. Bandow and Nils Metzler-Nolte
Chem. Sci., DOI: 10.1039/C4SC02709D, Edge Article

Non-classical β-carbonic anhydrase inhibitors-towards novel anti-mycobacterials
Natascha von Gnielinski, Lisa Nienaber, Lyndel Mason, Samantha Ellis, James A. Triccas, Rohan A. Davis and Andreas Hofmann
Med. Chem. Commun., DOI: 10.1039/C4MD00310A, Concise Article

Indole-based novel small molecules for the modulation of bacterial signalling pathways
Nripendra Nath Biswas, Samuel K. Kutty, Nicolas Barraud, George M. Iskander, Renate Griffith, Scott A. Rice, Mark Willcox, David StC. Black and Naresh Kumar
Org. Biomol. Chem., DOI: 10.1039/C4OB02096K, Paper

Synthesis, antiribosomal and antibacterial activity of 4′-O-glycopyranosyl paromomycin aminoglycoside antibiotics
Weiwei Chen, Takahiko Matsushita, Dimitri Shcherbakov, Heithem Boukari, Andrea Vasella, Erik C. Böttger and David Crich
Med. Chem. Commun., DOI: 10.1039/C4MD00119B, Concise Article

Antibacterial activity of adamantyl substituted cyclohexane diamine derivatives against methicillin resistant Staphylococcus aureus and Mycobacterium tuberculosis
Beena, Deepak Kumar, Widuranga Kumbukgolla, Sampath Jayaweera, MaiAnn Bailey, Torey Alling, Juliane Ollinger, Tanya Parish and Diwan S. Rawat
RSC Adv., DOI: 10.1039/C4RA00224E, Paper

N-Substituted 2-aminoimidazole inhibitors of MRSA biofilm formation accessed through direct 1,3-bis(tert-butoxycarbonyl)guanidine cyclization
Andrew A. Yeagley, Zhaoming Su, Kára D. McCullough, Roberta J. Worthington and Christian Melander
Org. Biomol. Chem., DOI: 10.1039/C2OB26469B, Paper

Development of ruthenium(II) complexes as topical antibiotics against methicillin resistant Staphylococcus aureus
P.-L. Lam, G.-L. Lu, K.-M. Hon, K.-W. Lee, C.-L. Ho, X. Wang, J. C.-O. Tang, K.-H. Lam, R. S.-M. Wong, S. H.-L. Kok, Z.-X. Bian, H. Li, K. K.-H. Lee, R. Gambari, C.-H. Chui and W.-Y. Wong
Dalton Trans., DOI: 10.1039/C3DT52879K, Paper

Synthesis and biological activity of novel bis-indole inhibitors of bacterial transcription initiation complex formation
Marcin Mielczarek, Ruth V. Devakaram, Cong Ma, Xiao Yang, Hakan Kandemir, Bambang Purwono, David StC. Black, Renate Griffith, Peter J. Lewis and Naresh Kumar
Org. Biomol. Chem., DOI: 10.1039/C4OB00460D, Paper

Potent growth inhibitory activity of (±)-platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis
Gamal A. I. Moustafa, Shoji Nojima, Yoshi Yamano, Akio Aono, Masayoshi Arai, Satoshi Mitarai, Tetsuaki Tanaka and Takehiko Yoshimitsu
Med. Chem. Commun., DOI: 10.1039/C3MD00016H, Concise Article

Thiazole-based aminopyrimidines and N-phenylpyrazolines as potent antimicrobial agents: synthesis and biological evaluation
Konstantinos Liaras, Athina Geronikaki, Jasmina Glamočlija, Ana Ćirić and Marina Soković
Med. Chem. Commun., DOI: 10.1039/C4MD00124A, Concise Article

Chlorido-containing ruthenium(II) and iridium(III) complexes as antimicrobial agents
Mallesh Pandrala, Fangfei Li, Marshall Feterl, Yanyan Mulyana, Jeffrey M. Warner, Lynne Wallace, F. Richard Keene and J. Grant Collins
Dalton Trans., DOI: 10.1039/C3DT32775B, Paper

Highly active antibacterial ferrocenoylated or ruthenocenoylated Arg-Trp peptides can be discovered by an L-to-D substitution scan
H. Bauke Albada, Pascal Prochnow, Sandra Bobersky, Julia E. Bandow and Nils Metzler-Nolte
Chem. Sci., DOI: 10.1039/C4SC01822B, Edge Article


Infection prevention and alternatives to address AMR


Books and Reviews:

Polymeric Materials with Antimicrobial Activity: From Synthesis to Applications
Alexandra Muñoz-Bonilla (Editor), María Cerrada (Editor), Marta Fernández-García (Editor)
ISBN (print): 978-1-84973-807-1, Copyright: 2013

Silver in Healthcare: Its Antimicrobial Efficacy and Safety in Use
Alan B. G. Lansdown (Author)
ISBN (print): 978-1-84973-006-8, Copyright: 2010

Photodynamic Inactivation of Microbial Pathogens: Medical and Environmental Applications
Michael R Hamblin (Editor), Giulio Jori (Editor)
ISBN (print): 978-1-84973-144-7, Copyright: 2011

Towards bacterial adhesion-based therapeutics and detection methods
Núria Parera Pera and Roland J. Pieters
Med. Chem. Commun., DOI: 10.1039/C3MD00346A, Review Article

Superhydrophobic surfaces for the reduction of bacterial adhesion
Xiaoxue Zhang, Ling Wang and Erkki Levänen
RSC Adv., DOI: 10.1039/C3RA40497H, Review Article

Nanosilver-based antibacterial drugs and devices: Mechanisms, methodological drawbacks, and guidelines
Loris Rizzello and Pier Paolo Pompa
Chem. Soc. Rev., DOI: 10.1039/C3CS60218D, Review Article


Original research articles:

Antimicrobial nanotechnology: its potential for the effective management of microbial drug resistance and implications for research needs in microbial nanotoxicology
Deborah M. Aruguete, Bojeong Kim, Michael F. Hochella, Yanjun Ma, Yingwen Cheng, Andy Hoegh, Jie Liu and Amy Pruden
Environ. Sci.: Processes Impacts, DOI: 10.1039/C2EM30692A, Critical Review

The promotion of antimicrobial activity on silicon substrates using a “click” immobilized short peptide
Lin Wang, Junjian Chen, Lin Shi, Zhifeng Shi, Li Ren and Yingjun Wang
Chem. Commun., DOI: 10.1039/C3CC47922F, Communication

An efficient strategy to achieve hydrophilic polymeric silver(I) materials with exceptional antibacterial activity
Sheng-Chun Chen, Zhi-Hui Zhang, Qun Chen, Li-Qun Wang, Juan Xu, Ming-Yang He, Miao Du, Xiao-Ping Yang and Richard A. Jones
Chem. Commun., DOI: 10.1039/C2CC36538C, Communication

Silver nanoparticle-embedded polymersome nanocarriers for the treatment of antibiotic-resistant infections
Benjamin M. Geilich, Anne L. van de Ven, Gloria L. Singleton, Liuda J. Sepúlveda, Srinivas Sridhar and Thomas J. Webster
Nanoscale, DOI: 10.1039/C4NR05823B, Paper

Antibacterial polymeric nanostructures for biomedical applications
Jing Chen, Fangyingkai Wang, Qiuming Liu and Jianzhong Du
Chem. Commun., DOI: 10.1039/C4CC03001J, Feature Article

Magnetic hybrid colloids decorated with Ag nanoparticles bite away bacteria and chemisorb viruses
Hye Hun Park, SungJun Park, GwangPyo Ko and Kyoungja Woo
J. Mater. Chem. B, DOI: 10.1039/C3TB20311E, Paper

Covalent attachment of multilayers (CAM): a platform for pH switchable antimicrobial and anticoagulant polymeric surfaces
Heather A. Pearson, Joseph M. Andrie and Marek W. Urban
Biomater. Sci., DOI: 10.1039/C3BM60238A, Paper

Multi-scale strategy to eradicate Pseudomonas aeruginosa on surfaces using solid lipid nanoparticles loaded with free fatty acids
Erik N. Taylor, Kim M. Kummer, Deepti Dyondi, Thomas J. Webster and Rinti Banerjee
Nanoscale, DOI: 10.1039/C3NR04270G, Paper

Bio-inspired resin acid-derived materials as anti-bacterial resistance agents with unexpected activities
Mitra S. Ganewatta, Yung Pin Chen, Jifu Wang, Jihua Zhou, Jerry Ebalunode, Mitzi Nagarkatti, Alan W. Decho and Chuanbing Tang
Chem. Sci., 2014, DOI: 10.1039/C4SC00034J, Edge Article

Antibacterial activity of Ionic Liquids based on ampicillin against resistant bacteria
Ricardo Ferraz, Vânia Teixeira, Débora Rodrigues, Rúben Fernandes, Cristina Prudêncio, João Paulo Noronha, Željko Petrovski and Luís C. Branco
RSC Adv., DOI: 10.1039/C3RA44286A, Paper

The surface charge of anti-bacterial coatings alters motility and biofilm architecture
Olena Rzhepishevska, Shoghik Hakobyan, Rohit Ruhal, Julien Gautrot, David Barbero and Madeleine Ramstedt
Biomater. Sci., DOI: 10.1039/C3BM00197K, Paper

Studies of the drug resistance response of sensitive and drug-resistant strains in a microfluidic system
Xiangdan Jiang, Yu Kang, Xingjie Pan, Jun Yu, Qi Ouyang and Chunxiong Luo
Integr. Biol., DOI: 10.1039/C3IB40164B, Paper

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Introducing MedChemComm Associate Editor Dr Matthew Fuchter

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.

Recent Publications:

Design, synthesis and initial characterisation of a radiolabelled [18F]pyrimidoindolone probe for detecting activated caspase-3/7
Org. Biomol. Chem., 2015, 13, 5418-5423, Paper

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors
Med. Chem. Commun., 2014, 5, 1821-1828, Concise Article
From themed collection Epigenetics

Perspectives on natural product epigenetic modulators in chemical biology and medicine
Nat. Prod. Rep., 2013, 30, 605-624, Review Article

Submit a manuscript for Matthew to handle

Visit Matthew’s Homepage


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Introducing new Editorial Board member – Professor Andrea Cavalli

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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MedChemComm’s new Editorial Board member – Professor Koen Augustyns

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.

Recent Publication:

Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold
Koen Jansen, Hans De Winter, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Anne-Marie Lambeir, Ingrid De Meester, Koen Augustyns and Pieter Van der Veken
DOI: 10.1039/C4MD00167B

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Chemistry in Health – Towards new therapeutics to fight disease

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.

This event is organised as part of our human health programme. You can find out more at http://rsc.li/global-challenges

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MedChemComm’s new Editorial Board member – Dr Mike Hann

Dr Mike Hann obtained his PhD in Organic chemistry at the City University in London in 1980 with Professor Peter Sammes. He then worked in the UK as a medicinal chemist at Roussel, Wyeth and GD Searle. During his time at GD Searle he had the opportunity to get involved with the emerging use of computational chemistry and molecular modelling in drug discovery.

He joined GlaxoSmithKline (GSK) at Greenford in 1986 as a computational chemist and after several mergers and a lot of fun science he became head of computational chemistry at GSK in the UK and then director of Biomolecular Sciences with responsibilities for x-ray crystallography, biophysics and protein mass spectrometry studies.

His current role continues to find him at the interface of chemistry and biology, where he says “all the interesting stuff happens!“, and involves promoting scientific exchange, excellence and innovation to improve drug discovery methodologies within GSK and with our external collaborators. He has published extensively on a wide range of subjects including the following highly cited publications. He is also a visiting adjunct professor in the department of chemistry at Imperial College London.

Past publications:

  • Hann, Michael M.; Keseru, Gyoergy M. Finding the sweet spot: the role of nature and nurture in medicinal chemistry. Nature Reviews Drug Discovery (2012), 11(5), 355-365.
  • Hann, Michael M. Molecular obesity, potency and other addictions in drug discovery. MedChemComm (2011), 2(5), 349-355.
  • Hann, Michael M.; Leach, Andrew R.; Harper, Gavin.  Molecular Complexity and Its Impact on the Probability of Finding Leads for Drug Discovery. Journal of Chemical Information and Computer Sciences (2001),  41(3),  856-864.
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