DP-9024

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Company:

Ono Pharmaceutical

Drug class:

GCN2 modulator, PERK modulator

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almost3years

DP-9024, an investigational small molecule modulator of the Integrated Stress Response kinase PERK, causes B-cell cancer growth inhibition as single agent and in combination with standard-of-care agents (AACR 2023)

The ISR/UPR is a targetable vulnerability in cancers with high basal levels of ER stress. DP-9024 increases UPR signaling via activating PERK dimerization. This novel mechanism leads to antitumoral effects in B-cell cancers in vitro and in vivo likely through the induction of unresolved ER stress, which may potentially provide an alternative mechanism to current UPR targeting therapies.

almost 3 years ago

Combination therapy

CASP3 (Caspase 3) • ATF4 (Activating Transcription Factor 4) • CASP7 (Caspase 7)

DP-9024

almost3years

Dimerization-induced activation of the integrated stress response kinase PERK by an investigational small molecule modulator, DP-9024 (AACR 2023)

Paradoxical stimulation of the ISR family member kinase PERK, through direct binding and dimerization by DP-9024, led to unresolved ER stress that can potentially be leveraged as a novel mechanism to induce growth arrest in UPR vulnerable cancers, including myelomas and B-cell lymphomas.

almost 3 years ago

PARP Biomarker

CASP3 (Caspase 3) • ATF4 (Activating Transcription Factor 4) • CASP7 (Caspase 7)

DP-9024