April 23-24, 2014

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Biologics have been useful in treating diseases of chronic inflammation such as multiple sclerosis or rheumatoid arthritis, but there is still an unmet medical need for more convenient and safer treatment options for such diseases. A few kinase inhibitors that fit these criteria have been recently launched and a few are in late-stage development. Join fellow drug discovery scientists at Cambridge Healthtech Institute’s fifth annual Anti-Inflammatories: Small Molecule Approachesday- and-a-half meeting track to stay abreast of the latest progress in the field of oral-based (mostly small molecules) inhibitors for inflammation. A focus will be on the chemical optimizations that have enabled the leading inflammation drug candidates to progress. Presentations on newer and non-kinase targets for combating inflammation will also be a part of the agenda.

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Protein-Protein Interactions

Targeting the non-catalytic site of protein-protein interactions (PPIs) with small molecules has enabled drug discovery to move beyond the typical enzyme targets such as proteases and kinases and address disease-state relevant regulatory complexes of biological processes such as intracellular signal transduction, transcription, immuno-modulation, epigenetic modifications and protein stability. However targeting PPIs pose unique challenges because the targets’ structure (an interaction site between two proteins) is often not known and is usually a larger area with different physico-chemical properties than a ‘catalytic site’. Cambridge Healthtech Institute’s seventh annual Protein-Protein Interactions meeting will highlight the different disease areas where targeting PPIs is showing promise and will bring colleagues together to discuss lead optimization challenges for the medicinal chemist. Hear case studies of PPI-targeted compounds that are progressing in drug development or not, with a focus on the kinds of roadblocks the compounds encountered.

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Epigenetic Inhibitor Discovery

Within the past few years, an expanding collection of epigenetic modulators - spanning multiple classes and disease implications - have been positioned as promising targets for therapeutic development. Since the approval of first-generation epigenetic therapies, an increasing amount of chemically tractable epigenetic targets, such as Histone Deacetylases (HDACs), Histone Methyltransferases (HMTs), Histone Demethylases (HDMs), and a distinct set of chromatin readers - the BET family bromodomains - have given rise to novel inhibitors that are now in preclinical and clinical development. However, obtaining potent, highly-selective and cell-active inhibitors requires skillful utilization of varied assays and screening methods, such as high-throughput screening (HTS), focused screening, knowledge/fragment-based approaches, and phenotypic assays to efficiently navigate lead discovery of epigenetic targets. Cambridge Healthtech Institute is proud to announce the inaugural Epigenetic Inhibitor Discovery conference, gathering a diverse cross-section of academic and industry leaders actively working on developing epigenetic inhibitors.


April 24-25, 2014

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Macrocyclics and Constrained Peptides

The main excitement over the newer synthetic/non-naturally occurring smaller macrocyclic molecules as drug candidates is their middle ground promise. Like traditional ‘small molecules,’ macrocyclic peptides can be delivered orally and pass through the cell membrane to reach intracellular targets. Yet they have some of the advantages of bigger molecules like biologics such as the ability to better disrupt protein-protein interactions while still allowing for high potency and specificity. Cambridge Healthtech Institute’s second annual Macrocyclics and Constrained Peptides Drug Discovery meeting will explore this emerging class of molecules (as well as constrained peptides that can be considered a subset of macrocyclic peptides) and the types of cellular targets they are being developed against. Case studies of macrocyclic compounds that originated from different types of libraries will also be presented with a focus on the types of chemical optimizations needed to progress from hits to lead candidates.

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Fragment-Based Drug Discovery

Fragment-based approaches for finding potential new medical therapies are now a part of many drug discovery programs. There are at least 25 disclosed drug candidates forging ahead in clinical development whose origins can be traced to fragment-based screening campaigns. However medicinal chemists, especially in larger companies with high throughput screening departments, have other sources for ‘hits’ to optimize into lead drug candidates. What is the exact role and usefulness of fragment-based screening nowadays? How is it changing? How can it be improved? How can it be better integrated or used synergistically with other approaches? Join your discovery chemistry peers at Cambridge Healthtech Institute’s ninth annual Fragment-Based Drug Discovery meeting to discuss these questions and hear presentations about the ever present challenge for medicinal chemists: optimization strategies to get to better drugs from fragment hits.


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Kinase Inhibitor Chemistry

The human kinome has proven to be a large class of chemically tractable drug targets, with a significant portion of drug development efforts geared toward the discovery and optimization of chemical matter modulating kinase activity. Yet, despite the hundreds of kinase inhibitors currently in discovery, preclinical and clinical phases, a relatively small subset of the kinome has been thoroughly explored with selective small molecule inhibitors. Thus, in this highly competitive space, continued success requires the identification of novel kinase targets, obtaining target selectivity and specificity, developing compounds with non-traditional mechanisms of inhibition - such as binding outside the ATP site or cyclic inhibitors - and applying kinase inhibitors to non-oncology indications. Cambridge Healthtech Institute’s fifth annual Kinase Inhibitor Chemistry will once again join academic and industry leaders to network, collaborate and discuss practical solutions to these challenges, while exploring the ever expanding arena of kinase drug discovery.