Emerging roles of PARP-1 driven dual inhibitors in cancer therapy: SAR-guided strategies and synthetic lethality.
1/5 보강
Poly (ADP-ribose) polymerase-1 (PARP-1) plays an important role in DNA damage repair and preservation of genomic integrity, making it promising target in oncology.
APA
Dhir R, Ghosh P, et al. (2026). Emerging roles of PARP-1 driven dual inhibitors in cancer therapy: SAR-guided strategies and synthetic lethality.. Future medicinal chemistry, 18(5), 599-614. https://doi.org/10.1080/17568919.2026.2619466
MLA
Dhir R, et al.. "Emerging roles of PARP-1 driven dual inhibitors in cancer therapy: SAR-guided strategies and synthetic lethality.." Future medicinal chemistry, vol. 18, no. 5, 2026, pp. 599-614.
PMID
41565349 ↗
Abstract 한글 요약
Poly (ADP-ribose) polymerase-1 (PARP-1) plays an important role in DNA damage repair and preservation of genomic integrity, making it promising target in oncology. PARP-1 inhibitors (PARP-1i) employ synthetic lethality to specifically target cells with deficiency in homologous recombination repair, such as those with BRCA1/2 mutation and other DNA impairments. Although PARP-1 inhibitors have shown clinical success, challenges like acquired resistance and limited efficacy are still matters of concern. Increasing evidence supports the potential of dual-targeting inhibitors that target PARP-1 along with other oncogenic drivers (e.g. HDAC, EGFR, and CDK) to amplify anti-proliferative activity and surmount resistance mechanism. This review comprehensively provides in-depth investigation of dual inhibitors in context to PARP-1, evaluating their design rationale, structure activity relationship (SARs), pharmacological properties, synthetic scheme, and more. By combining mechanistic insights with drug discovery, this work aims to create a road map for generating next-generation PARP-1 inhibitors, providing strategic recommendations in order to improve therapeutic efficacy and broaden clinical applicability across diverse cancer types.
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