BACKGROUND: Once a promising drug target is identified, the steps to actually discover and optimize a drug are diverse and challenging. OBJECTIVE: The goal of this study was to provide a road map to navigate drug discovery. METHODS: Review general steps for drug discovery and provide illustrating references. RESULTS: A number of approaches are available to enhance and accelerate target identification and validation. Consideration of a variety of potential mechanisms of action of potential drugs can guide discovery efforts. The hit to lead stage may involve techniques such as high-throughput screening, fragment-based screening, and structure-based design, with informatics playing an ever-increasing role. Biologically relevant screening models are discussed, including cell lines, 3-dimensional culture, and in vivo screening. The process of enabling human studies for an investigational drug is also discussed. CONCLUSIONS: Drug discovery is a complex process that has significantly evolved in recent years.
BACKGROUND: Once a promising drug target is identified, the steps to actually discover and optimize a drug are diverse and challenging. OBJECTIVE: The goal of this study was to provide a road map to navigate drug discovery. METHODS: Review general steps for drug discovery and provide illustrating references. RESULTS: A number of approaches are available to enhance and accelerate target identification and validation. Consideration of a variety of potential mechanisms of action of potential drugs can guide discovery efforts. The hit to lead stage may involve techniques such as high-throughput screening, fragment-based screening, and structure-based design, with informatics playing an ever-increasing role. Biologically relevant screening models are discussed, including cell lines, 3-dimensional culture, and in vivo screening. The process of enabling human studies for an investigational drug is also discussed. CONCLUSIONS: Drug discovery is a complex process that has significantly evolved in recent years.
Authors: Eric C Lau; Damian J Mason; Nicole Eichhorst; Pearce Engelder; Celestina Mesa; E M Kithsiri Wijeratne; G M Kamal B Gunaherath; A A Leslie Gunatilaka; James J La Clair; Eli Chapman Journal: Org Biomol Chem Date: 2015-02-28 Impact factor: 3.876
Authors: Xiaoyu Xia; Yu-Chen Lo; Ankur A Gholkar; Silvia Senese; Joseph Y Ong; Erick F Velasquez; Robert Damoiseaux; Jorge Z Torres Journal: ACS Chem Biol Date: 2019-05-08 Impact factor: 5.100