Author Archive

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

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

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.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

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!

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

8th BMCS PhD Biological and Medicinal Chemistry Symposium

On 12th Decemeber the Biological and Medicinal Chemistry Sector (BMCS) of the Royal Society of Chemistry  held its eighth postgraduate symposium for PhD students and postdoctoral workers researching in biological or medicinal chemistry and related areas. The day consisted of 11 oral presentations (8 student and 3 keynote) and poster session.

This year’s symposium was a great success with around 150 participants attending, with an excellent scientific standard all around.

The BMCS judges  awarded two prizes on the day; one for the best oral presentation and one for the best poster, with the winners recieving £300 and £150 respectively as well as each getting a year’s subscription to MedChemComm.

Congratulations go to:

Oral presentation winner:  Charlotte Sutherell, University of Cambridge for her talk “Bromodomain Inhibitor Development and Testing to Evaluate the Therapeutic Potential of SMARCA4 in SWI/SNF Mutant Cancers”

Poster winner: Niall Igoe, University College London for his poster on “Epigenetic Drug Discovery: Small Molecule Inhibitors of Class IV Bromodomains”

Oral presentation winner Charlotte Sutherell being presented with her award Poster prize winner Niall Igoie being presented with his award
Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Take 1…minute for chemistry in health

Can you explain the importance of chemistry to human health in just 1 minute? If you’re an early-career researcher who is up to the challenge, making a 1 minute video could win you £500.

The chemical sciences will be fundamental in helping us meet the healthcare challenges of the future, and we are committed to ensuring that they contribute to their full potential. As part of our work in this area, we are inviting undergraduate and PhD students, post-docs and those starting out their career in industry to produce an original video that demonstrates the importance of chemistry in health.

We are looking for imaginative ways of showcasing how chemistry helps us address healthcare challenges. Your video should be no longer than 1 minute, and you can use any approach you like.

The winner will receive a £500 cash prize, with a £250 prize for second place and £150 prize for third place up for grabs too.

Stuck for inspiration? Last year’s winning video is a good place to start. John Gleeson’s video was selected based on the effective use of language, dynamic style, creativity and its accurate content.

The closing date for entries to be submitted is 30 January 2015. Our judging panel will select the top five videos. We will then publish the shortlisted videos online and open the judging to the public to determine the winner and the runners up.

For more details on how to enter the competition and who is eligible, join us at the Take 1… page.

Good luck!

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Q2 Top Ten most accessed articles

During the months April – June 2014, the most downloaded MedChemComm articles were:

The synthesis and functional evaluation of a mitochondria-targeted hydrogen sulfide donor, (10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5- yl)phenoxy)decyl) triphenyl phosphonium bromide (AP39)
Sophie Le Trionnaire, Alexis Perry, Bartosz Szczesny, Csaba Szabo, Paul G. Winyard, Jacqueline L. Whatmore, Mark E. Wood and Matthew Whiteman
DOI: 10.1039/C3MD00323J

Emerging classes of armed antibody therapeutics against cancer
Christian Hess, Dario Venetz and Dario Neri
DOI: 10.1039/C3MD00360D

The role of modern drug discovery in the fight against neglected and tropical diseases
Jeremy N. Burrows, Richard L. Elliott, Takushi Kaneko, Charles E. Mowbray and David Waterson
DOI: 10.1039/C4MD00011K

Discovery of BET bromodomain inhibitors and their role in target validation
S. Müller and S. Knapp
DOI: 10.1039/C3MD00291H

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson
DOI: 10.1039/C3MD00386H

Ambient mass spectrometry technologies for the detection of falsified drugs
María J. Culzoni, Prabha Dwivedi, Michael D. Green, Paul N. Newton and Facundo M. Fernández
DOI: 10.1039/C3MD00235G

Affinity-based target identification for bioactive small molecules
Makoto Kawatani and Hiroyuki Osada
DOI: 10.1039/C3MD00276D

Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
Charlotte E. Allen, Amanda J. Welford, Thomas P. Matthews, John J. Caldwell and Ian Collins
DOI: 10.1039/C3MD00308F

Two diseases, one approach: multitarget drug discovery in Alzheimer’s and neglected tropical diseases
F. Prati, E. Uliassi and M. L. Bolognesi
DOI: 10.1039/C4MD00069B

FP tethering: a screening technique to rapidly identify compounds that disrupt protein–protein interactions
Jean M. Lodge, T. Justin Rettenmaier, James A. Wells, William C. Pomerantz and Anna K. Mapp
DOI: 10.1039/C3MD00356F

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Recent HOT MedChemComm articles

The following are HOT articles, as recommened by the reviewers of the articles. These have all been made free to access until 24th October:

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
Apirat Chaikuad, Andrew M. Petros, Oleg Fedorov, Jing Xu and Stefan Knapp
Med. Chem. Commun., DOI: 10.1039/C4MD00237G, Concise Article
From themed collection Epigenetics


Gold compounds as aquaporin inhibitors: new opportunities for therapy and imaging
Andreia de Almeida, Graça Soveral and Angela Casini
Med. Chem. Commun., DOI: 10.1039/C4MD00265B, Review Article


A novel surface-coated nanocarrier for efficient encapsulation and delivery of camptothecin to cells
Rie Wakabayashi, Ryutaro Ishiyama, Noriho Kamiya and Masahiro Goto
Med. Chem. Commun., DOI: 10.1039/C4MD00179F, Concise Article
From themed collection In celebration of Seiji Shinkai’s 70th Birthday


Peptide HIV fusion inhibitors: modifications and conjugations
Wei Liu, Jianjun Tan, Mohammadreza Mohammadzad Mehryar, Zhiping Teng and Yi Zeng
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00214H, Review Article


3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors
Craig J. Kutz, Steven L. Holshouser, Ethan A. Marrow and Patrick M. Woster
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00283K, Concise Article
From themed collection Epigenetics

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Medicinal Chemistry Residential School comes to Asia

With a 40 year history in the UK, the Royal Society of Chemistry Medicinal Chemistry Residential School has trained some of the world’s leading medicinal chemists working in the pharmaceutical industry. Now, for the first time, this highly successful course will be coming to Asia – from 20-23 November, Shangai, China.

Do you want to develop your medicinal chemistry skills?

This 3-day course strengthens excellence in medicinal chemistry by highlighting best practice and facilitating understanding of the factors governing modern drug discovery.

What you will learn

The course covers all aspects of drug discovery. A full list of themes is on our website. These topics will be explored through a varied programme of lectures, case histories, and hands-on tutorial sessions.

Who you will learn from

This is a truly unique opportunity for discussions and networking with peers and internationally recognised leaders in the field. See our list of prestigious speakers.

Registration is now open. There are limited spaces available on the course so make sure you register as soon as possible.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

RSC Organic Division Poster Symposium 2014

RSC Organic Division Poster Symposium 2014, headline sponsored by F. Hoffmann-La Roche, Ltd.

The poster symposium, for final year organic chemistry PhD students, will take place at The Royal Society of Chemistry, Burlington House, London on Monday 01 December 2014.

The symposium offers final year PhD students a chance to showcase their research to their peers, leading academics and industrial chemists, and is open to all branches of organic chemistry. The symposium has a tradition of being the most competitive and highly regarded organic chemistry symposium for PhD students in the UK and ROI and we would like to thank F. Hoffmann-La Roche, Ltd. for their generous support of the event.

There will be a first prize of £500, two runner-up prizes of £250, and a “selected by Industry Prize”. Industrial delegates will make this selection by considering the research’s potential for application in an industrial context; the winner will also receive a prize of £500.

Closing date for submissions is Wednesday 01 October 2014.
For more information and to submit your abstract go to http://rsc.li/organic-poster

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Make your journal work for you

Want to know about the latest research we publish in MedChemComm? Want to be told about upcoming themed issues, or the most read articles, or other journal news?

Here are a few ways you can stay in touch with us and all that is happening:

RSS Feed for MedChemCommMost recent articles

Be informed about the latest articles published on our website by adding us to your RSS Feed.


Issue alerts

Sign-up to MedChemComm issue alertsGet the table of contents of the latest issue of MedChemComm sent direct to you when we publish the issue.


News alerts

Register for MedChemComm news alertsBy joining our news alerts we can let you know about:

  • Up-coming themed collections (print & electronic)
  • Top Ten most accessed articles
  • Changes to our Editorial Board
  • Important news for the journal


Twitter

We can also be found on Twitter @MedChemComm, add us and say hello. MedChemComm twitter


And of course you can always come back to this blog to find out about our journal news.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)