RSC Medicinal Chemistry Blog

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

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.

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

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.

MedChemComm has new Editorial Board members.

Earlier this year we told you about some of the retirements from our Editorial Board, now we are pleased to introduce some new faces. We are delighted to welcome:

Professor Koen Augustyns (University of Antwerp, Belgium)
Dr Christopher Burns (Walter and Eliza Hall Institute of Medical Research, Australia)
Professor Andrea Cavalli (University of Bologna, Italy)
Dr Mike Hann (GlaxoSmithKline, UK)
Dr Yoshinori Ikeura (Takeda Pharmaceutical Company Ltd, Japan)

We will introduce them all individually in a series of blogs, starting with this one.

Dr Christopher Burns

Dr Christopher Burns obtained his PhD in Organic Chemistry at the University of Melbourne in 1990. Following postdoctoral work at Pennsylvania State University with Prof Ken Feldman, he joined Pfizer (UK) as a medicinal chemist. After 5 years Chris returned to Australia where he worked in the field of biosensors for use in drug discovery, first as a Research Fellow at The University of Sydney, and then with biotech company Ambri.

In 2001 Chris joined Melbourne biotechnology company Cytopia to establish and lead the medicinal chemistry team and in 2006 he became Research Director. Over this time Chris led the discovery of two compounds that entered clinical trial: the orally active vascular disrupting agent lexibulin and the dual JAK1/2 inhibitor momelotinib. The latter compound, now being developed by Gilead Sciences, is currently undergoing multiple Phase II and III trials.

In 2010 Burns joined the Walter and Eliza Hall Institute of Medical Research and has embarked on a number of medicinal chemistry and chemical biology projects currently underway. He is a Fellow of the Royal Australian Chemical Institute and an Honorary Research Associate, School of Chemistry, BIO21, University of Melbourne where he lectures on anticancer drug discovery.

Chris recently contributed to our Epigenetics themed issue with his work on:

‘Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition’
DOI: 10.1039/C4MD00182F

Chris’ homepage: http://www.wehi.edu.au/people/chris-burns