GPCR Drug Discovery
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, play a pervasive physiological and pathophysiological role in human. They are the leading therapeutic targets and have been of long-standing interest in the pharmaceutical industry. GPCR drug discovery is a complex, multistep process across different disciplines. In recent years, technological advances in revealing protein-protein interactions, structure determination and analysis, and developing specific antibodies and derivatives, have brought new opportunities for discovering drugs targeting both established and novel GPCR targets, and further improve our understanding and drug discovery capabilities.
Creative Biolabs provides professional services, innovative technologies and advanced platforms to accelerate GPCR drug discovery. Our experienced scientists offer the most robust services and one-stop solutions in a timely and cost-effective manner. We will work closely with our customers to help them overcome challenges.
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Target identification is the cornerstone of successful drug development. In view of the fact that the emergence rate of new drugs targeting GPCRs in the market is decreasing, there is a need to maintain high expectations for GPCR target identification. We provide customized services based on different approaches to help our customers accelerate target identification.
The failure of drug development is usually attributed to inadequate pre-clinical target validation. Early in-depth target validation can increase the understanding of the relationship between targets and diseases, thus increasing the possibility of clinical success. We provide our customers with reliable in silico target validation and biological target validation services to help them minimize project risks.
With the further elucidation of the regulatory mechanisms of diverse ligands on GPCR functions, the in-depth understanding of ligands has enabled the discovery of novel ligands, especially for orphan and understudied GPCRs that might be useful as therapeutic targets. We provide comprehensive services and one-stop solutions for identifying novel ligands that can selectively modulate the activity of GPCR targets with high efficacy.
Hit identification is the process of identifying compounds that can interact with validated targets. It is the first committed and most critical step for successful drug discovery. We provide different strategies to identify high-quality hits, maximize the number of initial hits, and accelerate the drug discovery progress with lower attrition rates.
Lead generation is a multi-dimensional process to optimize the properties of numerous hits. Before culminating in the identification of a preclinical candidate, the most promising lead compounds must undergo an optimization process to improve effectiveness, diminish toxicity and increase absorption. We are committed to helping our customers obtain high quality lead compounds to improve the success rate of drug development.
It is of great significance for drug design to study the interaction of biologically active compounds from the perspective of molecular structure or physical-chemical properties. The use of GPCR structures and new biophysical techniques offer new opportunities. We provide our customers with customized knowledge-driven design of drugs targeting GPCRs to meet their specific needs.
Anti-GPCR antibodies are practical tools to characterize GPCRs, especially orphan receptors. Monoclonal antibodies also show great potential as therapeutic drugs due to their superior specificity in regulating GPCRs to obtain the desired intracellular signaling. We provide the most robust and efficient services to help our customers overcome challenges in generating highly specific anti-GPCR antibodies.
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