Phenotypic Hit Discovery Oriented Workshop for Undergraduates: Integrating Cutting-Edge Knowledge and Discovery-Based Laboratory Experiences

A two-year long-term workshop centered around a phenotypicwhole-cellscreening strategy for integrating cutting-edge knowledge and discovery-basedlaboratory experiences was developed to serve as a preparatory coursefor enhancing the teaching quality of the upper-level discovery-basedresearch internship curriculum for pharmacy major undergraduates.The workshop comprises four modules that integrate lessons and experimentsinto a genuine research project, which initiates with a medicinal-chemistrycourse, run concurrently in the second year and culminates with thediscovery-based research internship curriculum for pharmacy majorstudents as a corequisite in the last year. The effective implementationof the featured pedagogical approaches in the modules is detailedas described. A group of students (N = 4) passed the instructor-studenttwo-way choice and were enrolled in the senior-level phenotypic hitdiscovery laboratory project. The students synthesized a small libraryof molecules, tested them in an antibacterial assay, and further designednew compounds to analyze structure-activity relationships.Furthermore, positive feedback from students revealed that the phenotypichit discovery oriented workshop enabled them to gain in-depth cutting-edgeknowledge and provided an understanding of how medicinal chemistsengage in new drug discovery research. The student's earlyexposure to troubleshooting or exploring unexpected results in anauthentic scientific environment inspired them with ambition and confidenceto engage with new drug discovery. We hope that this workshop willserve as a springboard for those wishing to educate medicinal chemistsat an undergraduate level with modern strategies that are relevantto the current and future drug discovery landscape.