Target intelligence / Profile preview

Cellular kinases and polymerases involved in cancer cell survival

Molecular classification
Enzyme, Kinase, Transferase, Polymerase, Receptor tyrosine kinase, Serine/threonine protein kinase
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Overview

This broad category refers to a diverse group of enzymes that are fundamental to the growth, maintenance, and stress resistance of malignant cells. Cellular kinases, including receptor tyrosine kinases (e.g., EGFR, HER2) and intracellular signaling kinases (e.g., PI3K, AKT, BRAF), function as molecular switches that relay growth signals and prevent programmed cell death (PubMed: 29149605). DNA polymerases and associated enzymes like PARP are critical for the rapid genomic replication and DNA damage repair required to sustain the high proliferative rate of tumors (UniProt: P15018). In oncology, these proteins are primary therapeutic targets; small-molecule inhibitors and monoclonal antibodies are used to block their activity, thereby inducing cell cycle arrest or apoptosis. However, the clinical utility of targeting these enzymes is often complicated by the emergence of bypass signaling pathways and secondary mutations that confer drug resistance (NIH: National Cancer Institute). Because many of these enzymes also perform essential functions in healthy tissues, therapeutic strategies must carefully balance efficacy against systemic toxicities such as immunosuppression and organ damage.

Other names
Oncogenic kinases and DNA replication enzymesSurvival-associated kinome and polymerase groupCancer-associated phosphotransferases and nucleotidyltransferases
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Mechanism of action

Inhibition of phosphate group transfer to protein substrates (kinases) or blocking the assembly of nucleotide polymers (polymerases) to disrupt oncogenic signaling and genomic integrity.

03

Biological functions

Signal transductionDNA replicationCell cycleDNA repairCell proliferationApoptosis evasion
04

Disease associations

Cancer
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Safety considerations

MyelosuppressionCardiotoxicityHepatotoxicityGastrointestinal toxicityAcquired drug resistanceOff-target inhibition of physiological signaling
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Interacting drugs

8 more in the full profile.

07

Biomarkers

BCR-ABL fusionEGFR mutation statusHER2/neu amplificationBRCA1/2 deficiencyKi-67 proliferation indexBRAF V600E mutation

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