Targeted chemical libraries: the keys to unlock the ubiquitin system Is novel chemistry the final frontier for ubiquitin system drug discovery? By Dr Jason Brown and Dr J. Mark Treherne
Although the widespread use of target-focused libraries has led to the rapid expansion of novel chemistry as research tools in drug discovery to exploit many classes of drug target, the ubiquitin system still remains a largely untapped medicinal chemistry opportunity.
Chemical space, high throughput screening and the world of blockbuster drugs. By Dr Hakim Djaballah Spring 2013
We are constantly told that if a high throughput screen does not identify hit(s) then blame it on the compounds in your library. The community has accepted this notion and unleashed a chemical space exploration through the use of novel or pre-existing synthetic chemistries to supposedly generate better ones.
Carbon-14 labelled API manufacturing. By Dr Sean L. Kitson and Dr David Speed Winter 2012/13
Carbon-14 labelled API and IMP requirements for Phase 0/I to Phase III mass balance and micro-dosing clinical trials can be met by contract manufacturing in compliance with MHRA and FDA Phase I cGMP guidelines. The short supply and escalating price of carbon-14 labelled building blocks has emphasised the demand for robust synthetic methodologies to incorporate the carbon-14 label efficiently into the API, and outsourcing to a CMO specialising in handling these challenges is a cost-effective approach. Further advantages accrue to clients by incorporation of these services within an overall drug development package, from discovery through to marketing.
Keeping ahead of the flow: Can the next generation of flow chemistry and biology platforms be fully integrated to transform the efficiency of small-molecule drug discovery for pharmaceutical industry? By Dr J Mark Treherne, Dr David M Parry and Christopher N Selway Summer 2011
There have been many false dawns in small-molecule drug discovery, promising individual technologies and integrated platforms to improve the efficiency of drug discovery. Although high-throughput screening, combinatorial chemistry and computational methods have all led to the rapid expansion of novel hit molecules and target-focused libraries, conventional medicinal chemistry is still the most effective way to optimise those early hits into the development compounds that can become drugs. This lengthy optimisation process is increasingly being outsourced to various locations worldwide with lower overheads and reduced long-term liabilities, as there has been no other expedient alternative to driving down costs to improve the earnings of pharmaceutical companies in the short term. However, effective integration and intelligent automation of the next generation of flow chemistry and biology technologies now has the real potential to transform this iterative process by enabling a step change in the efficiency, as well as a radical shortening of the timescales required to discover a candidate compound ready for development. It is envisaged by the authors that new small molecule integrated technology platforms will become sufficiently disruptive to challenge the efficiency of the latest monoclonal antibody discovery platforms.
Custom Carbon-14 Radiolabelling: investing to meet new challenges. By Dave Roberts Winter 2009
One consequence of an increasing demand from regulators for robust quantitative data on the behaviour of new drugs in man and for information on the fate of pharmaceuticals in the environment, has been an increase in demand for carbon-14 labelled compounds. This article focuses on the new uses for C-14 compounds, factors impacting on their preparation and how C-14 custom labelling suppliers are responding to meet new demands.
Overcoming the limitations of chemical structure. By Dr Andy Vinter, Dr Steve Gardner and Dr Sally Rose Summer 2009
The pharmaceutical business has been profoundly hampered by a ubiquitous and unexpected obstacles; the way it draws its chemical compounds. Scientists, patent agents and business decision makers from R&D, safety, and in-licensing are locked into a world of 2D atom and bond and Markush representations of the molecular structure of compounds.
Microwave-Assisted Orgainc Synthesis - an Enabling Technology with Disruptive Potential. By Dr Anil Vasudevan Fall 2008
Since the original publications on the benefits of conducting organic reactions in a microwave by Gedye1 and Majetich2 in the mid-80s, the uptake of this technique was sluggish at best for the next 12-14 years.
Zebrafish: a versatile in vivo model for drug safety assessment. Dr Wendy Alderton and Dr St phane Berghmans Fall 2006
Safety pharmacology has become an integral part of non-clinical safety assessment for new chemical entities in the past two decades1.The relative novelty of this discipline has granted it the flexibility to incorporate new experimental tools2.Telemetry has, for example, helped address the reduction of invasive methods in test animals and modern electrophysiological techniques have improved the assessment of cardiac safety 1.
Medicinal Chemistry: progress through innovation. By Dr Terry Hart Summer 2006
Medicinal chemistry is a specialised science that has evolved to encompass a broad range of disciplines concerned with the identification, synthesis and development of drug-like compounds for therapeutic use. It needs a wide range of expertise, developed through years of training, dedication and learning from best practices in order to produce drugs that are good enough to enter clinical trials in patients.
Microwave-assisted synthesis in the pharmaceutical industry a current perspective and future prospects. By Dr Richard Wagner Summer 2006
In the past five years there has been a dramatic upsurge in the use of microwave heating within the pharmaceutical industry to facilitate the chemical synthesis of new chemical entities.The increased uptake of this technology has been catalysed in part by the observation that reaction rates for the best cases could be accelerated 1,000-fold.
The Role of the Medicinal Chemist in the Drug Discovery Process: current status and future prospects. By Dr Stevan W Djuric Winter 2005
The need for the pharmaceutical industry to produce a constant stream of new NCEs has never been more paramount but with constantly changing R&D paradigms what is the role of the modern medicinal chemist? This article argues that with more versatility and the ability to work across various scientific disciplines the medicinal chemist will become a vital and, indeed, indispensable key to the future success of the industry.
Radiosynthesis; a vital role supporting drug development? By Dave Roberts and Professor Bill Lockley Fall 2004
The key in vivo drug metabolism and pharmacokinetic studies continue to be undertaken using radiolabelled versions of drug molecules. Traditionally, the preparation of these isotopically labelled compounds was largely the domain of specialist internal radiochemistry groups within large pharmaceutical companies (Big Pharma).
SCAVENGER strategies in organic synthesis. By Professor Peter Wipf and Dr Claire M. Coleman Spring 2004
Part 1 of this article (DDW,Winter 2003/4) discussed the fundamental principles of the use of scavenging techniques in combinatorial and organic synthesis. In this article, more recent developments are introduced that illustrate the broadening appeal of scavengers in organic chemistry. Specifically, the following topics are covered: Part 1: Polymeric scavengers; reactive filtration; ion exchange scavengers for product purification and sequestration enabling techniques. Part 2:Alternative resins; polyaromatic scavenger reagents; fluorous quenching scavenger protocols and microwave assisted scavenging protocols.
SCAVENGER strategies in organic synthesis. By Professor Peter Wipf and Dr Claire M. Coleman Winter 2003
Over the past 20 years combinatorial chemistry has proved to be an important tool for the generation of large numbers of compounds required for drug discovery programmes.This two-part article covers the history and current developments of scavenger strategies in combinatorial chemistry and organic synthesis.
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