Challenge: In recent years, only 8% of new oncology drugs have been approved for clinical use. One of the major challenges has been matching an appropriate therapeutic strategy to a cancer indication due to the heterogeneity of the disease. Nevertheless, the personalized medicine approach is not a simple process, as each cancer type represents a…
Challenge: Ion channels are involved in numerous physiological functions, and as drug targets have been implicated in a wide range of pathological conditions. However, despite considerable effort, channel-targeted drug discovery has been hampered by the absence of adequate tools to functionally screen molecules that can modulate channel activity. Solution: The researchers have developed an innovative…
Challenge: With the unique property of nuclear receptors (NRs) to directly interact with genomic DNA and control the expression of genes, nuclear receptors play key roles in both embryonic development and adult homeostasis as well as in many diseases. With a total of 48 different human receptors and 6 epigenetic-regulating cofactors identified, the is still…
Challenge: Membrane proteins, representing approximately one-third of all proteins in a cell, interact with each other and are responsible for a variety of processes, making them attractive therapeutic targets for many diseases such as hypertension, diabetes, neurological disorders and various cancers. In fact, membrane proteins represent 60% of all clinical drug targets, however, they are…
Challenge: Current therapies for heart failure primarily relieve symptoms, but most fail to correct organ dysfunction. New therapies, to target and improve cardiomyocyte function, are challenging to develop because of the complex functions of the heart muscle and the difficulty in modeling heart cell behavior. The same problems underlie the difficulty in assessing the cardiotoxic…
Challenge: G protein-coupled receptors (GPCRs) form the largest family of cell surface receptors involved in signal transduction of many hormones and transmitters. It follows that drugs targeting GPCRs represent close to 40% of all drugs on the market today. Recent discoveries regarding their function and mechanism of action help pave the way for the development…
Challenge: Because they are involved in so many physiological processes, G protein coupled receptors (GPCRs) are engaged by roughly 40% of marketed drugs and remain a prime target for the development of new therapeutics. To test the activity of drug candidates, understanding their action on their target in living animals is essential. However, this goal…
Challenge: One of the most promising strategies for discovering our future medications is via fragment-based lead discovery (FBLD). FBLD involves the screening of libraries of small molecules to first identify weak binders, essential to activate or inhibit a target protein involved in a particular disease. These binders are then synthetically matured to larger, more potent…
Challenge: G protein-coupled receptors (GPCRs) are the largest target class for approved drugs. Identification of new drug candidates has relied exclusively on high-throughput assays which track binding properties and are limited to a restricted number of signaling pathways. GPCRs are highly dynamic proteins that undergo numerous conformational changes upon receptor association with ligands and related…
Challenge: Proteins are the main effectors of cell activity and cardinal indicators of cell phenotype and response to stimuli such as drugs. Whereas sequencing technologies currently allow for broad and efficient genomic and transcriptomic profiling, multiplexed protein detection technologies are either prohibitively slow and expensive, limited in scope due to reagent cross-reactivity, or both. Critically,…