The Potential of PARP Inhibitors as Antitumor Drugs and the Perspective of Molecular Design DOI
Yinghan Wang, Jingtao Zhang, Xiaochen Wu

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 68(1), P. 18 - 48

Published: Dec. 26, 2024

PARP (poly-ADP ribose polymerase) has received widespread attention in cancer treatment. Research shown that plays a crucial role DNA damage repair and become popular target for drug design. Based on the mechanism of "synthetic lethality", multiple PARPis (PARP inhibitors) have been launched treatment BRCA deficient tumors. For example, approved significant potential treatment, particularly breast cancers associated with BRCA1/BRCA2 deficiencies. However, clinical efficacy safety inhibitors different remain issues cannot be overlooked. The design aims to eliminate their resistance broaden application scope. Designing selective PARP-1 is also strategy. PROTACs (Proteolysis Targeting Chimeras) degrade novel

Language: Английский

The Histomorphology to Molecular Transition: Exploring the Genomic Landscape of Poorly Differentiated Epithelial Endometrial Cancers DOI Creative Commons
Thulo Molefi, Lloyd Mabonga, Rodney Hull

et al.

Cells, Journal Year: 2025, Volume and Issue: 14(5), P. 382 - 382

Published: March 5, 2025

The peremptory need to circumvent challenges associated with poorly differentiated epithelial endometrial cancers (PDEECs), also known as Type II (ECs), has prompted therapeutic interrogation of the prototypically intractable and most prevalent gynecological malignancy. PDEECs account for cancer-related mortalities due their aggressive nature, late-stage detection, poor response standard therapies. are characterized by heterogeneous histopathological features distinct molecular profiles, they pose significant clinical propensity rapid progression. Regardless complexities around PDEECs, still being administered inefficiently in same manner clinically indolent readily curable type-I ECs. Currently, there no targeted therapies treatment PDEECs. realization new options transformed our understanding enabling more precise classification based on genomic profiling. transition from a provided critical insights into underlying genetic epigenetic alterations these malignancies. This review explores landscape focus identifying key subtypes mutations that variants. Here, we discuss how correlates outcomes can refine diagnostic accuracy, predict patient prognosis, inform strategies. Deciphering underpinnings led advances precision oncology protracted remissions patients untamable

Language: Английский

Citations

1

Liquid‒liquid phase separation and poly(ADP‒ribosyl)ation in the context of ultraviolet radiation-induced stress in mammalian cells DOI

Daniela Mejías,

Valentina Seballos, Laura Lafon-Hughes

et al.

Biophysical Reviews, Journal Year: 2025, Volume and Issue: unknown

Published: March 11, 2025

Language: Английский

Citations

1

Enhancing Radiation Therapy with PARP Inhibition in Soft Tissue Sarcomas: A Promising Synergy Requiring Specific Attention to Normal Tissues? DOI
Antonin Lévy, Céline Clémenson, Michele Mondini

et al.

Annals of Oncology, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 1, 2025

Language: Английский

Citations

0

The Potential of PARP Inhibitors as Antitumor Drugs and the Perspective of Molecular Design DOI
Yinghan Wang, Jingtao Zhang, Xiaochen Wu

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 68(1), P. 18 - 48

Published: Dec. 26, 2024

PARP (poly-ADP ribose polymerase) has received widespread attention in cancer treatment. Research shown that plays a crucial role DNA damage repair and become popular target for drug design. Based on the mechanism of "synthetic lethality", multiple PARPis (PARP inhibitors) have been launched treatment BRCA deficient tumors. For example, approved significant potential treatment, particularly breast cancers associated with BRCA1/BRCA2 deficiencies. However, clinical efficacy safety inhibitors different remain issues cannot be overlooked. The design aims to eliminate their resistance broaden application scope. Designing selective PARP-1 is also strategy. PROTACs (Proteolysis Targeting Chimeras) degrade novel

Language: Английский

Citations

2