Author Archive

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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Prof Richard Payne wins 2015 Emerging Investigator Lectureship

"It is a real honour to be awarded the MedChemComm Emerging Investigator Lectureship. I look forward to sharing some of our latest results at a conference later this year." Richard Payne, on winning the Lectureship

Congratulations to Professor Richard Payne from University of Sydney, Australia, the recipient of the 2015 MedChemComm Emerging Investigator Lectureship.

The annual MedChemComm Emerging Investigator Lectureship is given to a researcher who has made a significant contribution to medicinal chemistry research in the early part of their career. Nominations are received from members of the public and the recipient is chosen by a committee formed of members of the Editorial Board.

Richard will be presenting his lectureship at a conference of his choosing later this year.

About Richard

Richard Payne was born in Christchurch, New Zealand. He graduated from the University of Canterbury, New Zealand in 2002. In 2003 he was awarded a Gates Scholarship to undertake his PhD at the University of Cambridge, where he graduated with a PhD in 2006. After 18 months as a Lindemann Fellow at The Scripps Research Institute (La Jolla) he began his independent career (in January 2008) as a Lecturer in Organic Chemistry and Chemical Biology at The University of Sydney. Since 2015 he has been a Professor of Organic Chemistry and Chemical Biology and Australian Research Council Future Fellow at the University of Sydney.

Professor Payne’s research focusses on utilising the power of synthetic organic chemistry to interrogate biological systems and address problems of medical significance. He has made significant breakthroughs in the development of new methods for the chemical synthesis of biologically active modified proteins and in the discovery of novel lead compounds in the area of tuberculosis and malaria drug discovery.

As a result of his research endeavours he has been the recipient of several prestigious national awards including the Biota Medal in Medicinal Chemistry (2008), the Rennie Memorial Medal (2012), the Athel Beckwith Lectureship (2013), the Tregear Award for Peptide Science (2013), an Australian Research Council Future Fellowship (2013), the Le Févre Memorial Prize from the Australian Academy of Science, and now the 2015 MedChemComm Emerging Investigator Lectureship.

Some of Richard’s recent publications

Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents
Med. Chem. Commun., DOI: 10.1039/C4MD00406J, Concise Article
From themed issue New Talent: Asia-Pacific

Phosphate modulates receptor sulfotyrosine recognition by the chemokine monocyte chemoattractant protein-1 (MCP-1/CCL2)
Org. Biomol. Chem. DOI: 10.1039/C4OB02262A, Paper

Synthesis and immunological evaluation of self-adjuvanting MUC1-macrophage activating lipopeptide 2 conjugate vaccine candidates
Chem. Commun., DOI: 10.1039/C4CC03510K, Communication

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Antibiotic Resistance themed issue launched

We are pleased to announce an upcoming MedChemComm themed issue on Antibiotic Resistance. The Guest Editors for this issue are Professor Sylvie Garneau-Tsodikova (University of Kentucky, USA) and Professor Gerry Wright (McMaster University, Canada).

The scope of this issue is broad and encompasses, the mechanism of antibiotic resistance; discovery and development of novel antimicrobial agents; novel combination therapy; mechanism of action of novel antibiotics, and any other methods towards gaining a better understanding as well as combating bacterial infection and resistance to known antibiotics.

The deadline for submission is 18 August 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 Antibiotic Resistance.

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New Editorial Board Members for MedChemComm

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)
D
r 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

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From beehive to bone cement – a Chemistry World story

Taking inspiration from honey bees, scientists in South Korea have incorporated a compound used in beehives into a new strong biomaterial with sustained antimicrobial properties.

CAPE-loaded PMMA (left) was found to be stronger than gentamycin-loaded (right) PMMA

Bone cements have been used in surgery since the 1940s and work like a grout to fill the gaps between orthopaedic implants and bones. The most commonly used bone cements are made from a synthetic resin called poly (methyl methacrylate), or PMMA, and have recently been loaded with antibiotics, such as gentamycin, in an attempt to reduce healthcare related infections. However, the addition of antibiotics has raised concerns over antibiotic resistance, potential carcinogenic effects and the reduced mechanical strength of PMMA.

To overcome these potentially harmful limitations, a team led by Jeong Ho Chang at the Korea Institute of Ceramic Engineering and Technology, have developed PMMA bone cement loaded with caffeic acid phenethyl ester (CAPE). CAPE is an active component of bee propolis, a resin-like mixture collected by honey bees from various trees and buds and used to fill small gaps in the beehive. CAPE is thought to have antimicrobial, anti-inflammatory, antioxidant and anti-cancer effects and has already been approved for use in foods, drinks and cosmetics by the Food and Drug Administration.

The researchers were not only able to demonstrate that CAPE-loaded PMMA is an effective antimicrobial against Staphylococcus aureus, but it also has much better compressive strength than antibiotic-loaded PMMA. This impressive strength is thought to be due to a higher packing density caused by reinforced chemical bonding between the PMMA and CAPE through homogeneous loading. In contrast, conventional antibiotic-loaded bone cements are not uniformly mixed and have low loading efficiencies, so the compressive strength is similar to native PMMA. This also explains why CAPE–PMMA exhibits more controlled and sustained antimicrobial release compared to bone cement loaded with gentamycin.

Antoni Tomsia, a biomaterials expert specialising in treatments for bone defects and diseases at the Lawrence Berkeley National Laboratory, University of California, US, thinks that the incorporation of natural antimicrobials is a good idea. However, he emphasises that antimicrobial implants must go hand-in-hand with ‘provider hand hygiene, patient decolonisation efforts, or environmental decontamination, plus sterilisation, to prevent infections.’

Initial studies were carried out in rabbits and Chang believes that CAPE-loaded PMMA bone cement could be used for human clinical applications after therapeutic efficacy evaluation. ‘We are trying to discuss and work with a medical orthopaedics doctor and I think we can report the new clinical data in the near future,’ reveals Chang.

Story first appeared in Chemistry World November 2014, written by Thadchajini Retneswaran.

Hye Sun Lee and Jeong Ho Chang’s article entitled ‘Antimicrobial spine-bone cement with caffeic acid phenethyl ester for controlled release formulation and in vivo biological assessments‘ featured on the cover of issue 2 of MedChemComm

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Malcolm Campbell Memorial Prize winners 2015

The Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is proud to announce the winners of the Malcolm Campbell Memorial Prize for 2015. The prize has been awarded to Miles Congreve, Fiona Marshall and Malcolm Weir for the seminal contributions to G-protein-coupled receptor (GPCR) drug discovery made by Heptares Therapeutics Ltd since the company was founded in 2007.

This work has included building the world-renowned StaR© technology platform for X-ray crystallography of GPCRs and the invention of a number of clinical candidates. The winners are particularly commended on their outstanding publication record, and on their willingness to release data into the public domain.

The Malcolm Campbell Memorial prize commemorates Professor Campbell’s outstanding contributions in a broad range of chemistry and their applications to the understanding of bioactivity. The prize is awarded biennially and the 2015 prize will be presented formally to the winning team during the 18th RSC/SCI Medicinal Chemistry Symposium to be held at Churchill College in Cambridge on 13th to 16th September 2015.

The BMCS Committee wishes to express its gratitude for the high-quality entries from both academia and industry for the 2015 award.

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Changes to the Editorial Board

The turn of a new year brings with it several changes for MedChemComm and our Editorial Board.

Some members of the Editorial Board have reached the end of their terms as Editorial Board members and so have retired from their roles.

As of the 1st January 2015, Professor Gerhard Ecker, Dr David Rees, and Dr Uli Stilz have retired from the Editorial Board.

We would like to take this opportunity to thank David, Gerhard and Uli for all of their contributions to the journal over the past several years. Their invaluable input into the journal, since its launch in 2010, has been greatly appreciated.

We are pleased to say all three are keen to continue their support of MedChemComm and have accepted positions on our Advisory Board effective immediately. We look forward to continuing our relationship with them in their new roles.

Prof. Gerhard Ecker

Prof. Gerhard Ecker

Dr David Rees

Dr David Rees

Dr Uli Stilz

Dr Uli Stilz

Some new faces will be joining the team and more details on exactly who these are will be released shortly – so watch this space!

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