James Anson – Page 4 – RSC Medicinal Chemistry Blog

Author Archive

MedChemComm at conferences in 2014

24 Jan 2014

Dr Richard Kelly, Managing Editor

Dr Marie Cote, Deputy Editor

The MedChemComm team will be attending a number of conferences in 2014 and we would be delighted to meet you there.

We’re also the team behind MedChemComm’s sister journals Organic & Biomolecular Chemistry , Natural Product Reports, and the latest addition to the portfolio, Toxicology Research, so we’ll happily discuss your interdisciplinary research work. In fact, many of our authors choose to publish their research across all of these titles.

Here are just some of the conferences where you can meet us in the coming months:

GRC marine natural products 2-7 March Ventura, CA, USA – Meet Rich

Society of Toxicology annual meeting 23-27 March Phoenix, USA – Meet Marie

National Organic Symposium Trust 11-14 April Agra, India – Meet Rich

ISMSC-9 7-11 June Shanghai, China – Meet Marie

GRC Bioorganic Chemistry 8-13 June Proctor Academy, USA – Meet Rich

BOSS XIV 13-18 July Louvain-la-Neuve, Belgium – Meet Marie

Fall ACS meeting 10-14 August San Francisco, USA – Meet Rich

Gregynog Young Chemists’ Workshop 10-12 September Gregynog, Wales – Meet Marie

EFMC-ISMC 7-10 September Lisbon, Portugal – Meet Rich

Eurotox 7-9 September Edinburgh, UK – Meet Marie

Let us know if you are planning on attending any of these meetings, as we would be happy to meet you there!

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MedChemComm call for papers: Epigenetics themed issue

14 Jan 2014

MedChemComm themed issue: Epigenetics

Guest Editors: Dr Mark Bunnage (Pfizer) and Prof. James E. Bradner (Harvard Medical School)

Submission Deadline: 16^th June 2014

Submissions are now open for a high-profile themed issue on Epigenetics. The scope of the issue covers all areas of epigenetics within medicinal chemistry.

New research in MedChemComm is published as Concise Articles: flexible articles that have no strict page limits or formatting requirements. Manuscripts can be submitted in any reasonable format using our submission system. Template is not required. Please indicate that it is for the Epigenetics themed issue in the comments to the editor field. The level of quality of this issue will be high, and all manuscripts will undergo the journal’s normal peer review process.

The deadline for submissions to the themed issue is 16^th June 2014, although submissions before this date are of course welcomed.

If you would like to contribute to this issue please contact the Editorial Office.

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A Focus On Computer-Aided Drug Discovery

12 Dec 2013

A recent workshop on the role of computer aided drug discovery was jointly held by the Royal Society of Chemistry and the Biochemical Society with the aim of aiding collaborations between biological scientists and computational chemists.

Following this workshop we have brought together a collection of articles and books that highlight recent research on computer-aided drug discovery and related areas. Below is a slection from across the Royal Society of Chemistry and you can also find a collection of articles from the Biochemical Society HERE…

All of the Communications, Papers and Reviews below are free to access until 7 February 2014.

Books
(PDFs of the front matter, table of contents and first chapter are free to view.)

Physico-Chemical and Computational Approaches to Drug Discovery
Editors: Javier Luque, Xavier Barril

Drug Design Strategies
Editors: David J Livingstone, Andrew M Davis

Innovations in Biomolecular Modeling and Simulations: Volume 2:

Chapter 11 – Structure-based Design Technology CONTOUR and its Application to Drug Discovery
Zhijie Liu, Peter Lindblom, David A. Claremon and Suresh B. Singh

Chapter 12 – Molecular Simulation in Computer-aided Drug Design: Algorithms and Applications
Robert V. Swift and Rommie E. Amaro

Chapter 13– Computer-aided Drug Discovery: Two Antiviral Drugs for HIV/AIDS
J. Andrew McCammon

G Protein-Coupled Receptors: From Structure to Function:

Chapter 18 – Structure-based Virtual Screening for Ligands of G Protein-coupled Receptors
Stefano Costanzi

Reviews

Informatic strategies for the discovery of polyketides and nonribosomal peptides
Chad Johnston, Ashraf Ibrahim and Nathan Magarvey
Med. Chem. Commun., 2012, DOI: 10.1039/C2MD20120H, Review Article

Molecular docking for virtual screening of natural product databases
Dik-Lung Ma, Daniel Shiu-Hin Chan and Chung-Hang Leung
Chem. Sci., 2011, DOI: 10.1039/C1SC00152C, Minireview

Approaches to discover non-ATP site kinase inhibitors
Lori Krim Gavrin and Eddine Saiah
Med. Chem. Commun., 2013, DOI: 10.1039/C2MD20180A, Review Article

Drug repositioning by structure-based virtual screening
Dik-Lung Ma, Daniel Shiu-Hin Chan and Chung-Hang Leung
Chem. Soc. Rev., 2013, DOI: 10.1039/C2CS35357A, Review Article

Selective inhibition of the unfolded protein response: targeting catalytic sites for Schiff base modification
Susana M. Tomasio, Heather P. Harding, David Ron, Benedict C. S. Cross and Peter J. Bond
Mol. BioSyst., 2013, DOI: 10.1039/C3MB70234K, Review Article

Network-based drug repositioning
Zikai Wu, Yong Wang and Luonan Chen
Mol. BioSyst., 2013, DOI: 10.1039/C3MB25382A, Review Article

Communications and Papers

Virtual screening and experimental validation reveal novel small-molecule inhibitors of 14-3-3 protein–protein interactions
Philipp Thiel, Lars Röglin, Nicole Meissner, Sven Hennig, Oliver Kohlbacher and Christian Ottmann
Chem. Commun., 2013, DOI: 10.1039/C3CC44612C, Communication

Plugging the explicit σ-holes in molecular docking
Michal Kolář, Pavel Hobza and Agnieszka K. Bronowska
Chem. Commun., 2013, DOI: 10.1039/C2CC37584B, Communication

Fragments to link. A multiple docking strategy for second site binders
Márton Vass and György M. Keserű
Med. Chem. Commun., 2013, DOI: 10.1039/C2MD20267K, Concise Article

A rapid identification of hit molecules for target proteins via physico-chemical descriptors
Goutam Mukherjee and B. Jayaram
Phys. Chem. Chem. Phys., 2013, DOI: 10.1039/C3CP44697B, Paper

Discovery of novel inhibitors for human farnesyltransferase (hFTase) via structure-based virtual screening
Xiaojuan Yu, Xue Zhao, Lili Zhu, Chuanxin Zou, Xiaofeng Liu, Zhenjiang Zhao, Jin Huang and Honglin Li
Med. Chem. Commun., 2013,DOI: 10.1039/C3MD00058C, Concise Article

Prediction of chemical–protein interactions: multitarget-QSAR versus computational chemogenomic methods
Feixiong Cheng, Yadi Zhou, Jie Li, Weihua Li, Guixia Liu and Yun Tang
Mol. BioSyst., 2012, DOI: 10.1039/C2MB25110H, Paper

Identification of novel inhibitors of p53–MDM2 interaction facilitated by pharmacophore-based virtual screening combining molecular docking strategy
Weisi Wang, Xiaolei Zhu, Xueqin Hong, Lin Zheng, Hong Zhu and Yongzhou Hu
Med. Chem. Commun., 2013, DOI: 10.1039/C2MD20208E, Concise Article

Predicting cancer drug mechanisms of action using molecular network signatures
Justin R. Pritchard, Peter M. Bruno, Michael T. Hemann and Douglas A. Lauffenburger
Mol. BioSyst., 2013, DOI: 10.1039/C2MB25459J, Paper

Prospective use of molecular field points in ligand-based virtual screening: efficient identification of new reversible Cdc25 inhibitors
James C. Collins, Alan Armstrong, Kathryn L. Chapman, Hayley C. Cordingley, Albert A. Jaxa-Chamiec, Katie E. Judd, David J. Mann, Katherine A. Scott, Catherine J. Tralau-Stewart and Caroline M. R. Low
Med. Chem. Commun., 2013, DOI: 10.1039/C3MD00047H, Concise Article

Discovery of Rho-kinase inhibitors by docking-based virtual screening
Mingyun Shen, Huidong Yu, Youyong Li, Pixu Li, Peichen Pan, Shunye Zhou, Liling Zhang, Shang Li, Simon Ming-Yuen Lee and Tingjun Hou
Mol. BioSyst., 2013, DOI: 10.1039/C3MB00016H, Paper

Prediction of adverse drug reactions by a network based external link prediction method
Jiao Lin, Qifan Kuang, Yizhou Li, Yongqing Zhang, Jing Sun, Zhanling Ding and Menglong Li
Anal. Methods, 2013, DOI: 10.1039/C3AY41290C, Paper

Targeting the inactive conformation of protein kinases: computational screening based on ligand conformation
Pascal Bonnet, Daniel Mucs and Richard A. Bryce
Med. Chem. Commun., 2012, DOI: 10.1039/C1MD00256B, Concise Article

Structure-oriented bioinformatic approach exploring histidine-rich clusters in proteins
Shujian Cun, Yau-Tsz Lai, Yuen-Yan Chang and Hongzhe Sun
Metallomics, 2013, DOI: 10.1039/C3MT00026E, Concise Article

Rational design of small modified peptides as ACE inhibitors
Daniel G. Silva, Matheus P. Freitas, Elaine F. F. da Cunha, Teodorico C. Ramalho and Cleiton A. Nunes
Med. Chem. Commun., 2012, DOI: 10.1039/C2MD20214J, Concise Article

Development of a novel class of B-Raf^V600E-selective inhibitors through virtual screening and hierarchical hit optimization
Xiangqian Kong, Jie Qin, Zeng Li, Adina Vultur, Linjiang Tong, Enguang Feng, Geena Rajan, Shien Liu, Junyan Lu, Zhongjie Liang, Mingyue Zheng, Weiliang Zhu, Hualiang Jiang, Meenhard Herlyn, Hong Liu, Ronen Marmorstein and Cheng Luo
Org. Biomol. Chem., 2012, DOI: 10.1039/C2OB26081F, Paper

Computational design of a thermostable mutant of cocaine esterase via molecular dynamics simulations
Xiaoqin Huang, Daquan Gao and Chang-Guo Zhan
Org. Biomol. Chem., 2011, DOI: 10.1039/C0OB00972E, Paper

Structure determinants of indolin-2-on-3-spirothiazolidinones as MptpB inhibitors: An in silico study
Yinfeng Yang, Jinghui Wang, Yan Li, Wei Xiao, Zhenzhong Wang, Jingxiao Zhang, Weimin Gao, Shuwei Zhang and Ling Yang
Soft Matter, 2013, DOI: 10.1039/C3SM51995C, Paper

Synthesis of novel PPARα/γ dual agonists as potential drugs for the treatment of the metabolic syndrome and diabetes type II designed using a new de novo design program PROTOBUILD
Yushma Bhurruth-Alcor, Therese Røst, Michael R. Jorgensen, Christos Kontogiorgis, Jon Skorve, Robert G. Cooper, Joseph M. Sheridan, William D. O. Hamilton, Jonathan R. Heal, Rolf K. Berge and Andrew D. Miller
Org. Biomol. Chem., 2011, DOI: 10.1039/C0OB00146E, Paper

Anticancer loading and controlled release of novel water-compatible magnetic nanomaterials as drug delivery agents, coupled to a computational modeling approach
Pierre Dramou, Pengli Zuo, Hua He, Lien Ai Pham-Huy, Wenyue Zou, Deli Xiao, Chuong Pham-Huy and Theophilus Ndorbor
J. Mater. Chem. B, 2013, DOI: 10.1039/C3TB20502A, Paper

An NMR crystallography DFT-D approach to analyse the role of intermolecular hydrogen bonding and π–π interactions in driving cocrystallisation of indomethacin and nicotinamide
Dmytro V. Dudenko, Jonathan R. Yates, Kenneth D. M. Harris and Steven P. Brown
CrystEngComm, 2013, DOI: 10.1039/C3CE41240G, Paper

Modelling the possible bioactivity of ellagitannin-derived metabolites. In silico tools to evaluate their potential xenoestrogenic behavior
Luca Dellafiora, Pedro Mena, Pietro Cozzini, Furio Brighenti and Daniele Del Rio
Food Funct., 2013,4, DOI: 10.1039/C3FO60117J, Paper

Towards ab initio screening of co-crystal formation through lattice energy calculations and crystal structure prediction of nicotinamide, isonicotinamide, picolinamide and paracetamol multi-component crystals
H. C. Stephen Chan, John Kendrick, Marcus A. Neumann and Frank J. J. Leusen
CrystEngComm, 2013, DOI: 10.1039/C3CE40107C, Paper

You may also be interested in the upcoming Faraday Discussion on Molecular Simulations and Visualization in 2014 – Find out more here…

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Dr Ahmed Kamal joins the MedChemComm Advisory Board

29 Nov 2013

We are pleased to welcome Dr Ahmed Kamal to the Advisory Board of MedChemComm and look forward to working with him in the future.

Dr Kamal was born on 5th April, 1956 in Hyderabad, Andhra Pradesh, India. He obtained his Masters degree in 1977 and doctorate in 1982 from Aligarh Muslim University, India. From 1983 he has worked as a Scientist at the Indian Institute of Chemical Technology (IICT), Hyderabad, one of the leading chemical laboratories of the Council of Scientific and Industrial Research (CSIR), India. Between 1993 and 1994, he was a visiting scientist at the University of Alberta, Edmonton, Canada.

Since joining IICT, he has been involved in the pharmaceutical and medicinal chemistry of many different drug discovery programmes, both national and international, with excellent research outputs. Currently as well as being a leading scientist at IICT he is the Project Director of NIPER (National Institute of Pharmaceutical Education and Research), Hyderabad.

His current research interests revolve around multi-disciplinary research programmes including organic synthesis, medicinal, combinatorial and green chemistry, and chemical biology. Focussing on:

• The design and synthesis of gene-targeting compounds as new and novel anticancer agents

• New chemical entities for antitubercular and antimalarial activity

• The development of new efficient synthetic methodologies

Design, synthesis and biological evaluation of imidazo[1,5-a]pyridine–PBD conjugates as potential DNA-directed alkylating agents
Med. Chem. Commun., DOI: 10.1039/C2MD20219K, Concise Article

3-Diarylethyne quinazolinones: a new class of senescence inducers
Med. Chem. Commun., DOI: 10.1039/C2MD20302B, Concise Article

Synthesis of tetrazole–isoxazoline hybrids as a new class of tubulin polymerization inhibitors
Med. Chem. Commun., DOI: 10.1039/C2MD20085F, Concise Article

The first total synthesis of nhatrangin A
Org. Biomol. Chem., DOI: 10.1039/C3OB40252E, Paper

Inter- and intrastrand DNA crosslinks by 2-fluoro-substituted pyrrolobenzodiazepine dimers: stability, stereochemistry and drug orientation
Org. Biomol. Chem., DOI: 10.1039/C2OB25654A, Paper

Catalyst-free stereoselective cyclopropanation of electron deficient alkenes with ethyl diazoacetate
RSC Adv., DOI: 10.1039/C3RA42374C, Communication

An improved iron-mediated synthesis of N-2-aryl substituted 1,2,3-triazoles
RSC Adv., DOI: 10.1039/C3RA22485F, Paper

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4th CPA-RSC Symposium on Medicinal Chemistry: Epigenetics as Targets for Drug Discovery

14 Oct 2013

The RSC is jointly hosting a Medicinal Chemistry symposia on epigenetics as targets for drug discovery, comprising of two events:

4th CPA-RSC Symposium on Medicinal Chemistry: Epigenetics as Targets for Drug Discovery
Shandong University, Jinan, 2-3 November 2013

RSC International symposium on Epigenetics
Shanghai Institute of Materia Medica, 5 November 2013

The symposia will focus on epigenetics as targets for drug discovery, including trends and frontiers in epigenetics and histone modulators. It will feature a mix of high-profile international speakers and Chinese speakers from both academia and industry.

4^th CPA-RSC Symposium on Medicinal Chemistry: Epigenetics as Targets for Drug Discovery:

The 2013 Chinese Medicinal Chemistry Symposium (CMCS) and the 4^th CPA-RSC Symposium on Medicinal Chemistry: Epigenetics as Targets for Drug Discovery will be held from November 2 to 3, 2013 in Jinan, China. It is co-sponsored by Medicinal Chemistry Professional Committee of Chinese Pharmaceutical Association and Royal Society of Chemistry, and organized by Shandong University.

The symposium aims to provide a platform for medicinal chemists to exchange research information, discuss challenges, promote collaboration, and facilitate the transfer of new technologies. This symposium will showcase cutting-edge and complementary medicinal chemistry approaches ranging from complex natural products to small molecule fragments

Speakers include:

Chun-Wa Chung, GlaxoSmithKline, Stevenage, UK
Paul Brennan, SGC Oxford, UK
Qi Jun, Harvard Medical School, USA
Paul Thompson, Scripps Research Institute, Florida, USA
Erik De Clerq, Katholieke Universiteit Leuven, Belgium
Luo Cheng, Shanghai Institute of Materia Medica, China
Lu Xianping, Chipscreen Biosciences Ltd, China
Y. George Zheng, University of Georgia, USA
Zhang Mingqiang, Regional Associate Editor MedChemComm and VP Amgen, Shanghai, China
Hao Fang, Shandong University, China
David James, Royal Society of Chemistry, UK

RSC International symposium on Epigenetics:

This event will be hosted by Professor Jingkang Shen. If you are interested in attending this event, please email Dr Qingqing Qi with your contact details and email address.

Speakers include:

Chun-Wa Chung, GlaxoSmithKline, Stevenage, UK
Paul Brennan, SGC Oxford, UK
Qi Jun, Harvard Medical School, USA

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RSC Organic Division Poster Symposium: Deadline for poster abstracts 02 October 2013

23 Sep 2013

RSC Organic Division Poster Symposium: Deadline for poster abstracts 02 October 2013

The RSC Organic Division Poster Symposium is still accepting abstracts, but not for long. If you are a final year PhD student based in the UK/ROI and would like the opportunity to showcase your work to leading chemists in industry and academia, as well as your peers, make sure you submit your poster abstract by Wednesday 2^nd October.

The symposium will take place on Monday 2^nd December 2013, at The Chemistry Centre, Burlington House, London and there are several prizes available on the day. Alongside the £500 First Prize, there will also be a £500 “Selected by Industry” prize and two runners-up prizes of £250. And this year our headline sponsor, F. Hoffmann-La Roche are offering a further prize of a visit to their site in Basel, Switzerland, to the First and Industry prize winners.

Reasonable travel costs will be covered for the students who are selected to present at this meeting. If you would like to find out more about the symposium and submit an abstract, visit our symposium website

We would like to thank F. Hoffmann-La Roche, Ltd. for their generous support of this event.

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Christa E. Müller: MedChemComm’s new Associate Editor for Europe

16 Sep 2013

MedChemComm is delighted to welcome Professor Christa E. Müller (University of Bonn, Germany) as our new Associate Editor for Europe.

Christa is now accepting submissions so you can submit your next top research article to her!

Biography

Christa Müller studied pharmacy at the University of Tübingen, Germany, and received her Ph.D. in Pharmaceutical/Medicinal Chemistry from the same university. After a postdoctoral stay with John W. Daly (1989-1990 and 1992) at the Laboratory of Bioorganic Chemistry, National Institutes of Health, in Bethesda, Maryland, USA, she completed her habilitation thesis at the University of Tübingen in 1994, and became Associate Professor of Pharmaceutical Chemistry at Würzburg University in the same year. Since 1998 she is full professor of Pharmaceutical Chemistry at Bonn University. She is a co-founder of the Pharma-Center Bonn (www.pharmazentrum.uni-bonn.de), and has >250 publications in the field of medicinal chemistry and pharmacology.

Her scientific interests are focused on the medicinal chemistry and molecular pharmacology of purine-binding membrane proteins (purine receptors, ectonucleotidases) and lipid-activated orphan G protein-coupled receptors. Disease indications include neurodegenerative and inflammatory diseases and cancer. Her activities are ranging from basic research to collaborative drug development projects with pharma industry partners.

“MedChemComm has what it takes to become a leading journal of Medicinal Chemistry. It fills a gap since it differs from other med chem journals due to its wide scope and its unique format. I’m looking forward to seeing everyone’s exciting contributions and support!“

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Christa E. Müller

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Chemical and Biological Therapeutic Approaches to Neurological Disorders II

16 Sep 2013

There’s still time to register for the second one-day symposium on Chemical and Biological Therapeutic Approaches to Neurological Disorders, on Monday 23^rd September. The meeting will feature presentations and posters, from leading experts in academia and industry, about new developments in genetics, biochemistry, pathophysiology and medicinal chemistry relating to neurological disorders. A wide range of conditions will be discussed, including Alzheimer’s disease, epilepsy, schizophrenia, multiple sclerosis and Parkinson’s disease.

Neurological disorders are an increasingly important global public health problem, and the cause of much long-term suffering and disability. Currently available pharmaceuticals have been ineffective in curing many of these disorders and developing a deeper understanding of the nervous system is one of the major challenges facing scientists in the 21^st century. New research will hopefully contribute to the identification of better clinical biomarkers and medicines for diagnosis, monitoring and treatment of neurological disorders.

This one day symposium has been organised by the RSC’s Biotechnology Group with support from the Chemistry Biology Interface Division, and will be held at The Chemistry Centre, Burlington House, London. Speakers include:

Prof. Christopher Dobson, University of Cambridge
Prof. Ciaran Regan, University College Dublin
Prof. Lennart Bunch, University of Copenhagen
Prof. Peter Jenner, King’s College London
Prof. Stefan Przyborski, University of Durham
Dr. Jan Kehler, H. Lundbeck, A/S
Prof. Jonathan Corcoran, University College Dublin
Dr. Jan Passchier, Imanova Ltd.

If you would like to attend, please register here.

If you would like to find out more about this event, more information can be found on the RSC website.

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Drug-target residence time: introducing a web focus

13 Feb 2013

MedChemComm is delighted to present a concise web focus on drug-target residence time.

Koen Augustyns, Professor of Medicinal Chemistry at the University of Antwerp, Belgium, introduces the topic and has hand-picked 3 articles for this spotlight:

‘Analysis of drug-target residence time has begun to play a larger role in drug discovery as suggested by recent literature. For compounds with a slow off rate, long action at the target may render a perfect pharmacokinetic profile unnecessary, and selectivity vs. other targets inhibited only briefly may be more readily achieved. Specific, irreversible inhibition may be considered as the logical extreme for this approach. For other targets or therapeutic areas, other kinetic profiles may be desirable. The topic is timely as indicated by a recently launched Innovative Medicines Initiative project and the organization of several symposia exclusively focusing on this subject. However, there is a real need to build a better understanding in the medicinal chemistry and drug discovery community of the preferred profiles and screening methods for compounds with optimized drug-target residence times.’

In this MedChemComm web focus Georges Vauquelin comments on the determination of drug-target residence time by radioligand binding and functional assays and discusses their physiological relevance. Duncan C. Miller et al. investigate how molecular properties may affect the dissociation kinetics of ligand from its biological target. Finally, Juswinder Singh et al. describe the superiority of a novel EGFR targeted covalent inhibitor over its reversible analogues in overcoming drug resistance.

Interested? Why not read these three articles now:

Determination of drug–receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance
Georges Vauquelin
Med. Chem. Commun., 2012,3, 645-651
DOI: 10.1039/C2MD20015E, Review Article

Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target
Duncan C. Miller, Graham Lunn, Peter Jones, Yogesh Sabnis, Nichola L. Davies and Paul Driscoll
Med. Chem. Commun., 2012,3, 449-452
DOI: 10.1039/C2MD00270A, Concise Article

Superiority of a novel EGFR targeted covalent inhibitor over its reversible counterpart in overcoming drug resistance
Juswinder Singh, Erica Evans, Margit Hagel, Matthew Labinski, Alex Dubrovskiy, Mariana Nacht, Russell C. Petter, Aravind Prasad, Michael Sheets, Thia St Martin, Robert Tjin Tham Sjin, William Westlin and Zhendong Zhu
Med. Chem. Commun., 2012,3, 780-783
DOI: 10.1039/C2MD20017A, Concise Article

We hope that you find this selection interesting and stimulating to read – and why not submit your latest research in the area today!

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Methanocarba ring, the rigid ribose modification for purine and pyrimidine receptors

05 Feb 2013

Ribose containing adenosine receptors (ARs) and P2Y receptors for purine and pyrimidine nucleotides are involved in and regulate a myriad of physiological processes throughout the body, and have become important pharmaceutical targets for treating a diverse number of chronic and acute diseases.

An approach to enhance the selectivity of these nucleoside and nucleotide derivatives is to make the ribose ring more rigid. This is achieved by using a methanocarba (bicyclo[3.1.0]hexane) ring system as a rigid substitution for ribose which maintains either a North (N) or South (S) conformation, preserving or enhancing the potency and/or selectivity for certain receptor subtypes.

This review from Dilip K. Tosh and Kenneth A. Jacobson of the National Institute of Diabetes and Digestive and Kidney Diseases summarises recent advances in the synthetic approaches to methanocarba derivatives in the context of their use as definitive pharmacological probes.

Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches
Dilip K. Tosh and Kenneth A. Jacobson
DOI: 10.1039/C2MD20348K

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