Cytotoxic evaluation of YSL-109 in a triple negative breast cancer cell line and toxicological evaluations DOI
Yudibeth Sixto‐López, Cynthia Ordaz‐Pichardo, José A. Gómez-Vidal

et al.

Naunyn-Schmiedeberg s Archives of Pharmacology, Journal Year: 2023, Volume and Issue: 396(6), P. 1211 - 1222

Published: Jan. 25, 2023

Language: Английский

Unlocking the potential of novel Tetrahydro-β-Carboline-based HDAC6 inhibitors for colorectal Cancer therapy: Design, synthesis and biological evaluation DOI

Noreen Hemida,

Dalia S. El‐Gamil, Ahmed K. ElHady

et al.

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 108454 - 108454

Published: April 1, 2025

Language: Английский

Citations

0
The drug discovery candidate for targeting PARP1 with Onosma. Dichroantha compounds in Triple-negative breast cancer: A Virtual screening and Molecular Dynamic Simulation DOI
Mohamed J. Saadh,

Hanan Hassan Ahmed,

Radhwan Abdul Kareem

et al.

Computational Biology and Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 108471 - 108471

Published: April 1, 2025

Language: Английский

Citations

0
Challenging Triple Negative Breast Cancer through HDAC6 selective inhibition: novel cap-group identification, structure-activity relationships, computational and biological studies DOI Creative Commons
Simona Barone, Ivana Bello,

A Guadagni

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 292, P. 117634 - 117634

Published: April 18, 2025

Language: Английский

Citations

0
Transcriptomic landscapes underlying response and resistance to HDAC inhibitor chidamide in triple-negative breast cancer DOI Creative Commons
Yanxia Zhang,

Yunduo Liu,

Min Zhang

et al.

Genes & Diseases, Journal Year: 2025, Volume and Issue: unknown, P. 101676 - 101676

Published: May 1, 2025

Language: Английский

Citations

0
The combination of the HDAC1 inhibitor SAHA and doxorubicin has synergic efficacy in triple negative breast cancer in vivo DOI Creative Commons

Yuheng Pang,

Runze Shi,

Liujia Chan

et al.

Pharmacological Research, Journal Year: 2023, Volume and Issue: 196, P. 106926 - 106926

Published: Sept. 15, 2023

Vorinostat (SAHA) is a histone deacetylase inhibitor that exerts its effects through epigenetic regulation. Specifically, SAHA can inhibit the proliferation of triple-negative breast cancer (TNBC) cells alone or in combination with other chemotherapeutic agents. Doxorubicin (DOX), traditional drug, exhibits potent cytotoxic effect on while also inducing strong toxic effects. In this study, we investigated synergistic potential these two drugs against TNBC. Our results suggested could enhance inhibitory cell proliferation, resulting alterations mitotic phase, and suppression stemness. Moreover, our vivo study unveiled when was combined DOX, it not only exhibited an tumor metastasis but played role regulating immune microenvironment within tumors. Overall, DOX presents promising avenue for innovative chemotherapy context

Language: Английский

Citations

9
Synthesis and Biological Evaluation of a Series of Quinoline‐Based Quinazolinones and Carbamic Anhydride Derivatives DOI

Madhava Reddy Manne,

Rakesh R. Panicker,

K. Ramakrishnan

et al.

ChemistrySelect, Journal Year: 2023, Volume and Issue: 8(3)

Published: Jan. 18, 2023

Abstract Quinoline‐based compounds are one of the most important classes N ‐heterocyclics exhibiting a wide spectrum biological activities. There is constant demand for synthesis new quinoline‐based molecules suitable therapeutic applications. Here strategy developed to synthesize different quinazolinones catalytically using InCl 3 through cyclocondensation reaction isatoic anhydride and aniline with 2‐substituted‐quinoline‐3‐carbaldehyde produce 2‐(2‐phenoxyquinolin‐3‐yl)‐3‐phenyl‐2,3‐ dihydroquinazolin‐4(1H)‐one derivatives (>90 % yields). In contrast, reduced electrophilicity at metal center allows hydrazide ligand bind In(III) serendipitously forms benzoic(2‐phenoxyquinoline‐3‐carbonyl) carbamic (∼70 The mechanistic aspects these reactions were rationally explained. structure purity all isolated assessed by spectroscopic analytical data. view strong correlation existing between inflammation cancer progression, ex‐vivo anti‐inflammatory effect ligands was established. anti‐cancer property proposed delineated specific SIRT protein family. Further, computational docking studies on binding abilities 22 synthesized Sirt1 discussed in detail.

Language: Английский

Citations

8
Targeting neddylation and sumoylation in chemoresistant triple negative breast cancer DOI Creative Commons
Reid T. Powell, Amanda L. Rinkenbaugh,

Lei Guo

et al.

npj Breast Cancer, Journal Year: 2024, Volume and Issue: 10(1)

Published: May 27, 2024

Abstract Triple negative breast cancer (TNBC) accounts for 15–20% of cases in the United States. Systemic neoadjuvant chemotherapy (NACT), with or without immunotherapy, is current standard care patients early-stage TNBC. However, up to 70% TNBC have significant residual disease once NACT completed, which associated a high risk developing recurrence within two three years surgical resection. To identify targetable vulnerabilities chemoresistant TNBC, we generated longitudinal patient-derived xenograft (PDX) models from tumors before and after received NACT. We then compiled transcriptomes drug response profiles all models. Transcriptomic analysis identified enrichment aberrant protein homeostasis pathways post-NACT relative pre-NACT tumors. This observation correlated increased sensitivity vitro inhibitors targeting proteasome, heat shock proteins, neddylation pathways. Pevonedistat, annotated as NEDD8-activating enzyme (NAE) inhibitor, was prioritized validation vivo demonstrated efficacy single agent multiple PDX Pharmacotranscriptomic pathway-level correlation between pevonedistat activity post-translational modification (PTM) machinery, particularly involving sumoylation targets. Elevated levels both NEDD8 SUMO1 were observed exhibiting favorable compared those less vivo. Moreover, emerged expression neddylation-regulated tumor pevonedistat, indicating that these PTM may prove effective combating

Language: Английский

Citations

3
Epigenetic modifications: Critical participants of the PD‑L1 regulatory mechanism in solid tumors (Review) DOI Creative Commons
Xiaoran Ma, Jibiao Wu, Bin Wang

et al.

International Journal of Oncology, Journal Year: 2022, Volume and Issue: 61(5)

Published: Sept. 20, 2022

Immune checkpoint inhibitors targeting the programmed cell death protein 1 (PD‑1)/programmed ligand (PD‑L1) axis have achieved marked and durable efficacy in patients with different solid tumors improved their survival. However, presence of primary or acquired resistance to immune blockades results only a small fraction benefiting from treatment. An increasing number preclinical studies reported that PD‑L1 expression tumor cells is involved epigenetic changes, including histone modifications, non‑coding RNA regulation DNA methylation. In addition, multiple drugs been demonstrated directly indirectly interfere various cancer models. This provides opportunities better characterize regulatory mechanisms explore novel therapeutic strategies improve immunosuppressant response rates overcome drug resistance. The present review focuses on latest findings evidence mechanism regulating discusses biological clinical implications this tumors. A rational combination PD‑1/PD‑L1 blockade may prognosis

Language: Английский

Citations

13
Mitochondrial bioenergetics of breast cancer DOI

Tashvinder Singh,

Kangan Sharma,

Laxmipriya Jena

et al.

Mitochondrion, Journal Year: 2024, Volume and Issue: 79, P. 101951 - 101951

Published: Aug. 31, 2024

Language: Английский

Citations

2
Tackling Triple Negative Breast Cancer with HDAC inhibitors: 6 is the isoform! DOI Creative Commons

A Guadagni,

Simona Barone, Antonella Ilenia Alfano

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 279, P. 116884 - 116884

Published: Sept. 16, 2024

Language: Английский

Citations

2