What question did this study set out to answer?

To evaluate the antitumor effects of a new inhibitor targeting ADAR1 p150, focusing on its efficacy in high interferon melanoma.

Abstract 1559: First-in-class Zα-domain-targeted ADAR1 p150 inhibitor demonstrates potent antitumor efficacy in high IFN syngeneic melanoma

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Novel Zα-domain-targeted ADAR1 p150 inhibitor shows potent antitumor effects, indicating promising implications for cancer therapy.

To evaluate the antitumor effects of a new inhibitor targeting ADAR1 p150, focusing on its efficacy in high interferon melanoma.
Identified ADAR1 p150 inhibitors using a high-throughput binding assay and confirmed Zα domain binding via FRET assay.
Assessed anti-tumor efficacy in B16F10 melanoma mouse model as monotherapy and alongside anti-PD-1 therapy.
Explored ADAR1 p150 inhibitors as payloads for PD-L1-targeted antibody-drug conjugates.
Discovered a series of small-molecule inhibitors of ADAR1 p150 with submicromolar affinity.
Inhibited tumors showed significant anti-tumor activity, with nanomolar EC50 values in vivo.
Combined treatment with AVA-ADR inhibitors and anti-PD1 showed additive efficacy, exceeding single-agent response.
Tumor samples exhibited increased expression of interferon-stimulated genes and T-cell activation markers.

Kulkarni et al. (2026) studied this question.

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View Full Paper

Ask AI

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Authors

Novel Zα-domain-targeted ADAR1 p150 inhibitor shows potent antitumor effects, indicating promising implications for cancer therapy.

To evaluate the antitumor effects of a new inhibitor targeting ADAR1 p150, focusing on its efficacy in high interferon melanoma.
Identified ADAR1 p150 inhibitors using a high-throughput binding assay and confirmed Zα domain binding via FRET assay.
Assessed anti-tumor efficacy in B16F10 melanoma mouse model as monotherapy and alongside anti-PD-1 therapy.
Explored ADAR1 p150 inhibitors as payloads for PD-L1-targeted antibody-drug conjugates.
Discovered a series of small-molecule inhibitors of ADAR1 p150 with submicromolar affinity.
Inhibited tumors showed significant anti-tumor activity, with nanomolar EC50 values in vivo.
Combined treatment with AVA-ADR inhibitors and anti-PD1 showed additive efficacy, exceeding single-agent response.
Tumor samples exhibited increased expression of interferon-stimulated genes and T-cell activation markers.

Kulkarni et al. (2026) studied this question.

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