Biological Signalling Molecules & Major Clases of Drug Targets

Question 1

Difference between endo/exogenous and exogenous antagonist

Answer 1

Endogenous agonist: substance naturally produced in the body and activate receptor

Exogenous agonist: substance introduced from outside the body and activate receptor

Exogenous antagonist: substance introduced from outside the body and blocks the receptor

Question 2

Examples of endo/exogenous agonist

Answer 2

Endo: adrenaline, dopamine
Exo: synthetic compounds, drugs, toxins

Question 3

Four classifications of drugs targets

Answer 3

RITE

Receptor
Ion channel
Transporter
Enzyme

Question 4

Categories of endocrine and paracrine signalling molecules

Answer 4

Endocrine: Catecholamines, Peptides & proteins, Steroids

Paracrine: Peptide/polypeptide, Amines, Steroids, Glycoproteins

Question 5

Describe the main features of the four major groups of endocrine hormones

Answer 5

Peptide/polypeptides: all water soluble, large group

Amines: adrenal hormones are water soluble, thyroid hormones are lipid soluble

Steroids: all lipid soluble, derived from cholesterol

Glycoproteins: all water soluble,

Question 5

Describe the main features of the three major groups of paracrine hormones

Answer 5

Catechloamines:
Hydrophilic, causes change in membrane potential, triggers synthesis of cytotoxic 2’nd messengers

Peptides & Proteins:
Hydrophilic, triggers synthesis of cytotoxic 2’nd messengers, triggers protein kinase activity

Steroids:
Hydrophobic, receptor-hormone complex controls transaction.stability mRNAs

Question 6

RITE KLING to recall main classes of therapeutic drug tartlets

Answer 6

RITE: Receptor, Ion channel, Transporter, Enzymes

Receptors as drug targets can be further categorised into…

K(L)ING:
Kinase linked receptors
Ligand gated ion channels
Nucelar/intracellular
G-protein coupled receptors