Drug‐Receptor Interactions

Interação Fármaco-Recetor

Curse code:9494222

Carla Susana Silva Dias Reis Ascenso

Learning outcomes of the curricular unit:

The course is focused on the study of the basic principles of drug-receptor interactions, in a perspective that aims to develop knowledge and understanding of the relations between the chemical structure of a particular drug (or lead compound) and the resulting activity (structure-activity relationships, SAR). The biological targets for drug action will be reviewed, the pharmacophores of drugs or lead compounds established, and the effect on the biological activity of chemical substitutions concerning both pharmacophoric and non-pharmacophoric groups are discussed.

At the end of the course, students should be able:

• To identify the type of target that a given drug might have by recognition of specific features of its chemical structure
• To understand the pharmacological activity of known drugs at the molecular level
• To predict the activity that results by replacing specific chemical groups in a drug or a lead compound during a drug design and development approach

Syllabus:

1. PHYSICOCHEMICAL ASPECTS OF DRUG ACTION
2. DRUG-MEMBRANE PROTEIN RECEPTORS INTERACTIONS:
   Molecular mechanisms of drug action
3. DRUG-ENZYME INTERACTIONS:
   Molecular mechanisms of drug action 
   Active and allosteric sites for drug interaction 
   Structural aspects of enzymes affecting drug activity
4. DRUG-METALLOPROTEIN INTERACTIONS AND METALLODRUG-RECEPTOR INTERACTIONS:
   Properties of the essential metal ions and of the coordination compounds 
   Coordination chemistry 
   Metals in biological systems and metalloproteins action as drug targets 
   Metal containing drugs and metallodrug-receptor interactions
5. DRUG-NUCLEIC ACIDS INTERACTIONS:
   Molecular mechanisms of drug action and induced effects
6. DRUG-OTHER TARGETS INTERACTIONS:
   Drug action on receptors/target not covered on the topics above

The laboratory activities intent to demonstrate the basic concepts that support the theoretical ideas.

Suggested Bibliography:

• Patrick GL (2009) An introduction to medicinal chemistry, 4th ed., Oxford University Press. ISBN 0199234477
• Wermuth CG (2008) The practice of medicinal chemistry, 3rd ed., Elsevier Ltd. ISBN 9780123741943
• Nogrady T (2005) Medicinal chemistry – A molecular and biochemical approach, 3rd ed., Oxford University Press. ISBN 0195104560
• Kettle SFA (1998) Physical inorganic chemistry – a coordination chemistry approach. Oxford University Press. ISBN 0198504047
• Fraústo da Silva JJR, Williams RJP (1991) The biological chemistry of the elements – The inorganic chemistry of life. Oxford University Press. ISBN 0198558023