Molecular target 3 Flashcards
Difference between primary and secondary active transport
What are the different transporters
Pumps (transporters) can be divided into what four categories
Metabolite transporters
- 31 families
- Important drug target e.g. chloroquine
How do neurotransmitter transporters work
They transport vesicles containing neurotransmitters
- Vesicular inhibitory AA transporter
- Vesicular excitatory AA transporter
- Vesicular amine transporter
They are mainly used for scientific research
Neurotransmitter transporters name examples and where are they found
- They can be found in plasma membrane (presynaptic, postsynaptic and glial localisation)
How does citalopram work
- Its a seratonin/5-HT transporter
- Type of neurotransmitter transport (5-HT)
How does riluzole work
- EAAT; excitatory amino acid transport
Transporters as drugs
What an enzyme-coupled receptor
- Type of transmembrane receptor when bound by a ligand (growth factor or hormone) it functions as an enzyme
Classifications of ECRs
Receptor tyrosine kinases (main one)
Tyrosine kinase-associated receptors
Receptor serine/threonine kinases
Histidine-kinase-associated receptors
Receptor guanylyl cyclases
Receptor-like tyrosine phosphatases
Receptor tyrosine kinases
- Phosphorylate tyrosine residue on a specific set of substrates
- Usually activated by secrete growth factors and hormones
How are signals transduced across the plasma membrane? - ECR
- For GPCRs, ligands induce a conformational change
- Most ECRs are single a-helicase
- Receptor subunits create dimers or oligomers
- Oligomerisation of ECRs cause reorienation
- Reorientation - signalling- autophosphorylation
How does autophosphorylation cause biological effects?
- When a kinase enzyme adds a phosphate to itself
- This alters the enzymes structure and function
Why do we need to understand
molecular signalling pathway?
Identification of molecules involved in signalling may unearth new targets for drugs
EGF promotes cellular proliferation
Mutations in the EGF receptor have been identified in cancer
EGF and EGF-activated pathways are targets for anti-cancer therapies
Anti-EGF receptor antibodies
Tyrosine kinase inhibitors