Drug Screening

Recommended Prerequisites

Previous knowledge on Pharmacology and Moluclar and Cell Biology are recommended.

Teaching Methods

The teaching methods that will be used in this course unit include:

• Theoretical master classes with presentation of the syllabus by the Professor interspersed with flipped teaching;

• Practical-laboratory classes based on the execution of pharmacokinetic and pharmacodynamic screening methodologies explained in theoretical classes;

• Interpretation of results;

• Acquisition of concepts for processing data and respective statistical analysis, applying computer programs used during R&D programs;

• Preparation of reports regarding the practical-laboratory work.

Learning Outcomes

Upon completion of this course unit, the student should be able to:

• Identify the roles of pharmacological screening and localize it within R&D programs;

• Distinguish between pharmacodynamic and pharmacokinetic screening and integrate each one in the identification of hits and leads;

• Select and execute different in vitro methodologies that allow the evaluation of the pharmacokinetic properties of new drugs;

• Identify the types and objectives of primary assays and how are they chosen in accordance with the therapeutic target and the size of the compound library;

• Identify suitable molecular targets for the development of new centrally acting drugs and understand their relationship with the disease;

• Identify suitable molecular targets for the development of anti-inflammatory drugs and understand their relationship with the disease;

• Design a simple pharmacological screening test, applying the knowledge acquired.

Work Placement(s)

No

Syllabus

• Concepts/Definitions of Pharmacological Screening and methodologies of quality assessment;

• Pharmacokinetic screening models and techniques to estimate: intestinal absorption, permeability through the blood-brain barrier, binding to plasma proteins, metabolism;

• Assessment of drug-efflux transporter interaction (substrate, inhibitor, activator, inducer);

• Methods and methodos used for pharmacodynamic drug investigation in R&D processes;

• Molecular mechanisms and pharmacological targets in acute and chronic inflammatory diseases and screening methods of new chemical entities in their treatment;

• Molecular mechanisms and pharmacological targets in neurodegenerative diseases and screening methods of new chemical entities in their treatment;

• Practical-laboratory execution of the in vitro methodologies used to evaluate the pharmacological specificities mentioned above and critical interpretation of the results obtained.

Head Lecturer(s)

Ana Cristina Bairrada Fortuna

Assessment Methods

Assessment
Laboratory work or Field work: 30.0%
Exam: 70.0%

Bibliography

Brunton LL, Lazo JS, Parker KL (eds.) Goodman & Gilman’s The Pharmacological Basis of Therapeutics. McGraw-Hill, 11th Edition, 2006. ISBN 0-07-142280-3

Katzung B. G. (ed.) Basic and clinical Pharmacology. McGraw Hill, 9th edition, 2004. ISBN: 007-121931-5

Rang, Dale, Ritter & Flower. Rang & Dale's, Pharmacology. Churchill Livingstone, Elsevier, 6th Edition, 2007. ISBN: 978-0-443-06911-6.

A. N. Goktug, S. C. Chai, T. Chen. Data Analysis Approaches in High Throughput Screening. In Tech Open Science, 2013. Doi: 10.5772/52508.

A. Fortuna, et al. The importance of permeability screening in drug discovery process: PAMPA, Caco-2 and rat everted gut assays. Current Topics in Pharmacology. 2007; 11: 63-86

A. Fortuna, et al. Doi: 10.1111/j.1528-1167.2012.03409.x

A. Fortuna, el al. Doi:10.1002/jps.22796

A. Fortuna, et al. Doi. 10.1016/j.eplepsyres.2013.08.013.

J. Bicker, et al. Doi: 10.1016/j.ejps.2018.02.006

J. Bicker et al. Doi: 10.1124/dmd.117.077883

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