BIOM 3090 Lecture Notes - Lecture 3: Chronic Myelogenous Leukemia, Adipose Tissue, Imatinib
9 Jun 2018
School
Department
Course
Professor
Receptor
Tissue Localization
Action
β
1. Sinoatrial (SA) node of
heart
2. Cardiac muscle
3. Adipose tissue
1. Increase heart rate
2. increase contractility
3. increases lipolysis
β
1. bronchial smooth
muscle
2. gastrointestinal smooth
muscle
3. uterus
4. Bladder
5. Liver
6. Pancreas
1. Dilates bronchioles
2. Constricts sphincters and
relaxes gut wall
3. Relaxes uterine wall
4. Relaxes bladder
5. Increases
gluconeogenesis and
glycolysis
6. Increases insulin release
β
1. adipose tissue
1. increases lipolysis
- Transmembrane receptors with Enzymatic Cytosolic Domain
o Another major class of receptors are transmembrane receptors with
an intracellular linked enzymatic domain
o These receptors play an important role in cell metabolism, growth
and differentiation… tonic activation can cause tumours
o Consist of single membrane spanning proteins compared to the seven
membrane spanning G protein receptors
o Many of these receptors form dimers or multi subunit complexes to
transduce their signals
o Activity of these receptors includes adding/removing phosphate
groups from specific aa’s
▪ Phosphorylation of a protein can dramatically alter its energy
and shape, cause conformational changes
A. Receptor tyrosine kinases
a. Largest group of this receptor class
i. Endogenous ligands: insulin, PDGF, VEGF
ii. Effectors include SH2 domains on other signalling
molecules like Grb2
iii. Drugs: Imatinib (Gleevec®)-TK inhibitor
1. Anticancer agent: targets BCR-Abl TK;
underlies chronic myelogenous leukemia
B. Tyrosine Kinase-associated receptors
a. Includes cytokine receptors such as y-interferon
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