Target Validation

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Expression quantitative trait loci: present and future

Published by Philos Trans R Soc Lond B Biol Sci.

eQTLTarget ValidationTool

One of the most prominent directions has been the extensive set of studies on expression quantitative trait loci (eQTLs), namely, the discovery of genetic variants that explain variation in gene expression levels. Such studies have offered promise not just for the characterization of functional sequence variation but also for the understanding of basic processes of gene regulation and interpretation of genome-wide association studies. In this review, we discuss some of the key directions of eQTL research and its implications.

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MDC Connects: A Guide to Drug Discovery

Published by Medicines Discovery Catapult

Drug DiscoverySmall MoleculesTarget Identification

This guideline is a summary presentation from the Medicines Discovery Catapult (MDC) webinars. The aim was to create a resource of modern drug discovery knowledge to support small companies who are developing their own medicines. The guideline is focused on preclinical research with an emphasis on small molecules in the following topics:
• What makes, and how to identify, a good target
• Methods to identify the chemical compound which would become the drug
• How to optimise that drug
• How to test it works in models of disease
• And how to demonstrate that it would be safe to dose in humans

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Genetic-Driven Druggable Target Identification and Validation

Published by Trends Genet.

Expression Quantitative Trait LocusGenetic ToolboxGWAS AssociationTarget Identification

This article reviews the opportunities and challenges, and infer criteria for the optimal use of genetic findings in the drug discovery pipeline. Choosing the right biological target is the critical primary decision for the development of new drugs. Systematic genetic association testing of both human diseases and quantitative traits, along with resultant findings of coincident associations between them, is becoming a powerful approach to infer drug targetable candidates and generate in vitro tests to identify compounds that can modulate them therapeutically

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Drug discovery and development: Role of basic biological research

Published by Alzheimers Dement (N Y).

Drug DiscoveryTarget Validation

This article provides a brief overview of the processes of drug discovery and development. The aim is to help scientists whose research may be relevant to drug discovery and/or development to frame their research report in a way that appropriately places their findings within the drug discovery and development process and thereby support effective translation of preclinical research to humans.

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The Assay Guidance Manual

Published by NIH

Drug Discovery GuidelineDrug RepurposingNCATSNIHResearch and Drug DevelopmentSmall MoleculeTarget Validation Drug Development

This manual is a comprehensive resource for early drug discovery, providing guidelines for developing therapeutic hypotheses, validating targets and pathways, and establishing proof of concept criteria. It includes analyses of costs at various stages of drug development. The content encompasses critical decision-making points in New Chemical Entity (NCE) development, exploratory Investigational New Drug (IND) processes, and orphan drug designation. Furthermore, it delves into Drug Repurposing and drug delivery technologies, making it an invaluable guide for professionals initiating new drug discovery and development programs.

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