Tyrosine Kinase Mechanism
Tyrosine Kinases' cellular function
What is cell signaling?
BCR-ABL is known as a ____ gene
fusion
The first-line medication for CML
Imatinib
CML is the result of what genetic process?
Philadelphia chromosome t(9:22)
The types of bonds holding amino acids together
What are peptide bonds?
This type of TK responds to extracellular hormones.
What is receptor tyrosine kinase?
BCR-ABL protein is located in the....
What is the cytoplasm?
The second line medication for CML, and why is it more effective?
What is Dasatinib; higher binding affinity to BCR-ABL
What type of blood cells are typically elevated in CML
White blood cells
Are the phosphorylated Tyrosines in BCR-ABL toward or away from water?
Toward, since they are polar (hydrophilic)
Kinases are enzymes that couple the hydrolysis of ___ to the addition of a ___ group to its substrate.
ATP; phosphate
BCR-ABL is ______ active, or always on.
What is Constitutively active?
What type of kinetic inhibitor is imatinib and dasatinib?
Competitive inhibitor
______ is a hallmark symptom of CML typically identified in the physical exam
Splenomegaly
This amino acid resists helical structuring
Proline
The enzyme responsible for deactivating tyrosine kinases'.
Phosphatase enzyme
no, since it is a cytosolic protein.
The main reason for CML drug resistance is a decrease in sensitivity to imatinib caused by _____ or _____ of the BCR-ABL gene.
Mutation; Amplification. (ie 3 copies of BCR-ABL translocation in 4 out of 20 cells)
Inactive
What level of protein structure is responsible for BCR's multifunctional role to initiate signaling with actin, DNA, etc.
Quaternary structure