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Introduction and GPCR's

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Undergraduate BMS 301 Mind Map on Introduction and GPCR's, created by Kristi Brogden on 10/11/2014.
Kristi Brogden
Mind Map by Kristi Brogden, updated more than 1 year ago
Kristi Brogden
Created by Kristi Brogden about 11 years ago
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Resource summary

Introduction and GPCR's
  1. Targeting receptors
    1. Why target receptors?
      1. receptors = Proteins that signal following activation (Drug binding)
        1. Easier than trying to penetrate membrane
          1. Specific unlike ubiquitous proteins
            1. Less off target effects
          2. Small molecule drugs
            1. Targets
              1. Proteins
                1. Interested in proteins that naturally bind ligands
                  1. E.g. Receptors
                    1. E.g. kinases
                      1. Have regulatory domains
                      2. E.g. enzymes
                        1. Have substrate binding sites
                    2. Lipids
                      1. Polysaccharides
                        1. Nucleic acids
                      2. GPCR's are a good target
                      3. Asthma
                        1. Symptoms
                          1. shortness of breath, especially breathing out, cough
                            1. Inflammation of the airways
                              1. Bronchial hyper-reactivity
                                1. Reversible airways obstruction
                                  1. Worse in late phase
                                    1. More damaging in long term
                                      1. Lead to permanent damage in lungs
                                    2. Anti-asthmatic drugs
                                      1. Bronchodilators (salbutamol)
                                        1. Polymorphisms in β2- adrenoceptors associated with reduced efficacy of bronchodilators
                                        2. Anti-inflammatory agents (prednisolone & omalizumab)
                                          1. Steroids
                                            1. Have side effects
                                              1. Not good to take long term
                                                1. Prednisolone
                                                2. Omalizumab
                                                  1. Biological
                                                    1. Monoclonal antibody
                                                      1. Targets antibodies responsible for allergy
                                                      2. Very expensive so restricted to most severe cases
                                                    2. Abuse of inhalers
                                                      1. Hard to minimise
                                                        1. Receptors become desensitised
                                                          1. Would be better if we could minimise this
                                                      2. Designing new drugs for asthma
                                                        1. What do we need to consider?
                                                          1. Understand the disease
                                                            1. Identify receptors that may be involved
                                                              1. Understand receptors
                                                                1. Expression
                                                                  1. Structure
                                                                    1. Signalling
                                                                      1. Function
                                                                    2. Potential off target effects and toxicity
                                                                      1. Model system
                                                                        1. Not people
                                                                          1. Dangerous
                                                                          2. Not animals
                                                                            1. Unethical
                                                                              1. Expensive
                                                                              2. Cell line expressing receptor of interest
                                                                                1. What to measure
                                                                                  1. Binding
                                                                                    1. Fits receptor?
                                                                                    2. Downstream signalling
                                                                                      1. Use an assay that quantifies this signalling
                                                                          3. GPCR's
                                                                            1. Families
                                                                              1. Features
                                                                                1. FRET analysis of GPCRs

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