Protein Kinases as Drug Targets

A set of flashcards covering key vocabulary related to protein kinases as drug targets, including inhibitors, mechanisms of resistance, and structural features.

Kinase

An enzyme that catalyzes the transfer of phosphate groups from ATP to specific substrates, typically proteins.

ATP-Competitive Inhibitor

A type of drug that competes with ATP for binding to the active site of a kinase.

Gate Keeper Residue

An amino acid residue that plays a critical role in defining the size and accessibility of the binding site in kinases.

Specificity Pocket

A region in a kinase that determines the binding of inhibitors and can affect selectivity.

Therapeutic Resistance

The ability of cancer cells to resist the effects of a drug after initial treatment.

Functional Redundancy

The phenomenon where multiple kinases can perform similar functions, affecting the efficacy of inhibitors.

Covalent Inhibitor

An inhibitor that forms a permanent bond with a kinase, typically by reacting with specific amino acid residues.

Allosteric Inhibitor

A type of inhibitor that binds to a site other than the active site, altering the enzyme's activity.

Kinome

The complete set of protein kinases in a genome.

Selectivity Profile

A description of how selectively a kinase inhibitor targets specific kinases compared to others.

Binding Assay

A laboratory method used to measure the binding interactions between an inhibitor and a kinase.

Dissociation Constant (Kd)

A measure of the affinity of an inhibitor for its target; lower Kd values indicate higher affinity.

Lapatinib

An example of a dual kinase inhibitor used in breast cancer therapy, targeting HER2 and EGFR.

Gleevec (Imatinib)

A targeted therapy for chronic myelogenous leukemia that inhibits the BCR-ABL fusion protein.

EGFR

Epidermal Growth Factor Receptor, a protein that, when mutated, can lead to cancer cell growth and resistance to inhibitors.

Herceptin (Trastuzumab)

A monoclonal antibody that targets HER2 and is used in the treatment of breast cancer.

Phosphorylation

The addition of a phosphate group to a protein or other organic molecule, often activating/deactivating the target.

Kinase Inhibition Mechanism

The process by which a drug prevents a kinase from phosphorylating its substrates.

Mutation Resistance Mechanism

A way cancer cells can become resistant to drugs through genetic mutations altering the target site.

Cancer Pathway Independence

When cancer cells can grow without signals that typically regulate growth, often due to mutations.

Combination Therapy

Using more than one treatment method, such as multiple drugs, to improve efficacy against cancer.