BPS2022 - Drug discovery and design - 2019

6 points, SCA Band 2, 0.125 EFTSL

Undergraduate - Unit

Refer to the specific census and withdrawal dates for the semester(s) in which this unit is offered.

Faculty

Pharmacy and Pharmaceutical Sciences

Chief examiner(s)

Assoc. Professor Bernard Flynn

Coordinator(s)

Assoc. Professor Bernard Flynn

Unit guides

Offered

Parkville

  • Second semester 2019 (On-campus)

Prerequisites

BPS1022 Medicinal chemistry II: Reactivity and biomolecules

Notes

The computational component of BPS2022 is a modified form of teaching activities in PSC2142

Synopsis

This unit will educate students on different approaches in drug discovery and design: how bioactive molecules are identified and how these can be further modified structurally to improve their performance as safe and effective therapeutics: Sources of bioactive molecules: natural products, compound libraries (screening sets), endogenous ligands, computer aided drug-design; Hit-to-lead and lead-to-drug optimisation: modifying molecular structure for optimal performance (safety and efficacy).

Outcomes

After completing this unit, students will be able to:

  1. Demonstrate an understanding of different processes by which bioactive molecules can be identified, such as the screening of compound libraries, natural products and modifications of endogenous biomolecules, amongst others.
  2. Utilise different computational techniques to aid the design of small molecules with good affinity for biomolecular targets.
  3. Propose modifications to hit molecules necessary to map their structure-activity relationship (SAR). Utilise SAR maps in hit-to-lead and lead-to-drug optimisation.
  4. Design a series of assays (assay cascade) necessary for the optimisation of hit molecules into safe, efficacious drug molecules.
  5. Critically evaluate different drug discovery approaches and identify the most suitable approach for a particular situation.

Assessment

End-of-semester examination (50%) and in-semester assessment (50%)

Workload requirements

  • Twenty-four 1 hour lectures
  • Six 4-hour laboratories
  • Six 2-hour workshops

See also Unit timetable information

Additional information on this unit is available from the faculty at:

After completing this unit, students will be able to: (1) Demonstrate an understanding of different processes by which bioactive molecules can be identified, such as the screening of compound libraries, natural products and modifcations of endogenous biomolecules, amongst others. (2) Utilise different computational techniques to aid the design of small molecules with good affinity for biomolecular targets. (3) Propose modifications to hit molecules necessary to map their structure-activity relationship (SAR). Utilise SAR maps in hit-to-lead and lead-to-drug optimisation. (4) Design a series of assays (assay cascade) necessary for the optimisation of hit molecules into safe, efficacious drug molecules. (5) Critically evaluate different drug discovery approaches and identify the most suitable approach for a particular situation.