AL 17.3: PDGFR and Regulation

Question 1

what is the significance of PDGF

Answer 1

angiogenesis, mesenchyhmal stem cell differentiation, and repair

Question 2

How many members are in the class of PDGF and their respective PDGFR

Answer 2

1) PDGF-A, B, C, D
2) PDGF must dimerize
3) there are two (A, B) PDGFReceptors
4) PDGFR are RTK

Question 3

what is the significance of D842V in PDGFRa

Answer 3

1) D842V mutation encode a faulty tyrosine kinase intracellular domain of the PDGFRa RTK
2) D842V mutation changes affinity of phosphorylation
3) a drug that inhibits PDGFRa phosphorylation (imitinib) will be ineffective

Question 4

What are strategies to suppress PDGFR signaling

Answer 4

1) Block PDGF binding to its receptor (PDGFR)
a) antibody
b) aptamer
c) soluble receptor
2) Block PDGFR
a) antibody
b) dominant negative ligand (antagonist)
3) Block PDGFR function
a) kinase inhibitor
4) Silence the promoter sequence in PDGFR gene