Target intelligence / Profile preview

Proviral integration site for Moloney murine leukemia virus kinase (PIM kinase)

Target
PIM kinase
Molecular classification
Enzyme, Serine/threonine protein kinase, Proto-oncogene
01

Overview

PIM kinases (Proviral integration site for Moloney murine leukemia virus kinases) are a family of serine/threonine protein kinases, including three isoforms: PIM1, PIM2, and PIM3. They were originally identified as common proviral integration sites in Moloney murine leukemia virus-induced lymphomas. PIM kinases regulate cell cycle progression, survival, and proliferation by phosphorylating substrates involved in oncogenic signaling pathways. Overexpression of PIM kinases has been observed in various cancers, such as prostate, breast, colon, and pancreatic cancer, and is associated with poor prognosis. These kinases are considered attractive therapeutic targets, and several small-molecule inhibitors and protein degradation strategies (PROTACs) are under preclinical and clinical investigation; no drugs targeting PIM kinases are currently approved. PIM kinases are generally non-essential in non-malignant cells, suggesting potential for targeted cancer therapy with limited toxicity[2].

Other names
PIM kinaseProto-oncogene serine/threonine-protein kinase Pim-1Pim-1 kinasePIM1PIM2PIM3Proto-oncogene proteins PIM
02

Mechanism of action

Inhibition of kinase catalytic activity (ATP-competitive inhibition), PROTAC-mediated proteolysis (targeted protein degradation)

03

Biological functions

Cell proliferationCell survivalSignal transductionOncogenesisApoptosis resistance
04

Disease associations

CancerOncogenesisResistance to chemotherapy
05

Safety considerations

Drug resistance due to PIM kinase stabilityOn-target hematologic effects (theoretical, as clinical use not widely established)Off-target kinase inhibition
06

Interacting drugs

Protein kinase inhibitors

2 more in the full profile.

07

Biomarkers

PIM1/PIM2/PIM3 expression (as a potential marker for cancer progression or therapeutic response)

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