Published: Jan. 1, 2024
Language: Английский
Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(15), P. 12984 - 13018
Published: July 23, 2024
Triple-negative breast cancer (TNBC) remains a treatment challenge and requires innovative therapies. Hsp90, crucial for the stability of numerous oncogenic proteins, has emerged as promising therapeutic target. In this study, we present optimization Hsp90 C-terminal domain (CTD) inhibitor
Language: Английский
Citations
7
Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(1), P. 118 - 118
Published: Jan. 17, 2025
Background/Objectives: The synthesis of (E)-1-(1,3-diphenylallyl)-1H-1,2,4-triazoles and related compounds as anti-mitotic agents with activity in breast cancer was investigated. These were designed hybrids the microtubule-targeting chalcones, indanones, aromatase inhibitor letrozole. Methods: A panel 29 synthesized examined by a preliminary screening estrogen receptor (ER) progesterone (PR)-positive MCF-7 cells together cell cycle analysis tubulin polymerization inhibition. Results: (E)-5-(3-(1H-1,2,4-triazol-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-1-en-1-yl)-2-methoxyphenol 22b identified potent antiproliferative compound an IC50 value 0.39 mM cells, 0.77 triple-negative MDA-MB-231 0.37 leukemia HL-60 cells. In addition, demonstrated sub-micromolar range against NCI 60 line including prostate, melanoma, colon, leukemia, non-small lung cancers. G2/M phase arrest induction apoptosis inhibition demonstrated. Immunofluorescence studies confirmed that targeted while computational docking predicted binding conformations for colchicine site tubulin. Compound also selectively inhibited aromatase. Conclusions: Based on results obtained, these novel are suitable candidates further investigation cancer.
Language: Английский
Citations
0
International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 140437 - 140437
Published: Jan. 1, 2025
Language: Английский
Citations
0
Future Oncology, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 9
Published: Feb. 28, 2025
Breast cancer (BC) is the most common cause of leptomeningeal disease (LMD) and second brain metastases (BMs) among all solid malignancies. Both BMs LMD are associated with high morbidity mortality treatment options limited. Trastuzumab deruxtecan (T-DXd), an antibody drug conjugate combining a HER2-targeting topoisomerase I inhibitor, has shown activity in HER2-positive (HER2[+]) HER2-low tumors both preclinical clinical settings. Similarly, T-DXd efficacy HER2[+] BC patients central nervous system (CNS) involvement. However, data on and/or using TUXEDO-4 international, multicenter, single-arm, two-stage optimal Simon's design, phase II trial (NCT06048718) that will recruit total 27 adult (13 first stage, 14 stage depending responses stage) to evaluate metastatic population presenting newly diagnosed or progressing BM without type LMD.
Language: Английский
Citations
0
BMC Cancer, Journal Year: 2025, Volume and Issue: 25(1)
Published: April 14, 2025
The quality control testing component and main active ingredient of Polygonum multiflorum Thunb. (P. multiflorum), known as trans-2,3,5,4'-tetrahydroxystilbene 2-O-β-D-glucopyranoside (TSG), exhibits diverse biological activities. In this study, we report, for the first time, potent ability TSG to induce ferroptosis in triple negative breast cancer (TNBC) cell lines inhibit proliferation TNBC cells. Treatment with triggers production lipid peroxides, 4-hydroxynonenal (4-HNE), reactive oxygen species (ROS) cells, indicating induction ferroptosis. Both vivo vitro experiments confirmed inhibitory effects on metastasis. Furthermore, investigated other stilbene glycoside oligomers, alongside TSG, lines. These compounds also demonstrated suppress cells' findings suggest that by related could potentially serve a promising therapeutic strategy treatment.
Language: Английский
Citations
0
Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(11), P. 8473 - 8480
Published: May 28, 2024
ADVERTISEMENT RETURN TO ARTICLES ASAPPREVEditorialNEXTWomen's Healthcare: Call for ActionWendy B. Young*Wendy Young*[email protected]More by Wendy Younghttps://orcid.org/0000-0001-9584-6233Cite this: J. Med. Chem. 2024, XXXX, XXX, XXX-XXXPublication Date (Web):May 28, 2024Publication History Received14 May 2024Published online28 2024https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c01135https://doi.org/10.1021/acs.jmedchem.4c01135editorialACS Publications© 2024 American Chemical Society. This publication is available under these Terms of Use. Request reuse permissions free to access through this site. Learn MoreArticle Views-Altmetric-Citations-LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum full text article downloads since November 2008 (both PDF and HTML) across all institutions individuals. These metrics regularly updated reflect usage leading up last few days.Citations number other articles citing article, calculated Crossref daily. Find more information about citation counts.The Altmetric Attention Score a quantitative measure attention that research has received online. Clicking on donut icon will load page at altmetric.com with additional details score social media presence given article. how calculated. Share Add toView InAdd Full Text ReferenceAdd Description ExportRISCitationCitation abstractCitation referencesMore Options onFacebookTwitterWechatLinked InRedditEmail (2 MB) Get e-AlertscloseSUBJECTS:Cancer,Cancer therapy,Infectious diseases,Neurophysiology,Pharmaceuticals e-Alerts
Language: Английский
Citations
3
Published: Aug. 14, 2024
Triple-negative breast cancer (TNBC) lacks the expression of estrogen receptors, human epidermal growth factor receptor 2, and progesterone receptors (PR). TNBC has poorest prognosis among subtypes is more likely to respond immunotherapy due its higher PD-L1 a greater percentage tumor-infiltrating lymphocytes. Immunotherapy revolutionized treatment, especially with FDA's approval pembrolizumab (Keytruda) combined chemotherapy for advanced cases, opening new avenues treating this deadly disease. Although, can significantly improve patient outcomes in subset patients, achieving desired response rate all remains an unmet clinical goal. Strategies that responses immune checkpoint blockade, including combining chemotherapy, molecularly targeted therapy, or radiotherapy may rates outcomes. In review, we provide short background on explore different types strategies are currently being evaluated TNBC. Additionally, review why combination be beneficial, overview strategies, discuss novel immunotherapeutic opportunities approved near future
Language: Английский
Citations
3
Phytomedicine, Journal Year: 2024, Volume and Issue: 135, P. 156130 - 156130
Published: Oct. 5, 2024
Language: Английский
Citations
2
Cancers, Journal Year: 2024, Volume and Issue: 16(19), P. 3250 - 3250
Published: Sept. 24, 2024
Triple-negative breast cancer (TNBC) lacks the expression of estrogen receptors (ERs), human epidermal growth factor receptor 2 (HER2), and progesterone (PRs). TNBC has poorest prognosis among subtypes is more likely to respond immunotherapy due its higher PD-L1 a greater percentage tumor-infiltrating lymphocytes. Immunotherapy revolutionized treatment, especially with FDA’s approval pembrolizumab (Keytruda) combined chemotherapy for advanced cases, opening new avenues treating this deadly disease. Although can significantly improve patient outcomes in subset patients, achieving desired response rate all remains an unmet clinical goal. Strategies that enhance responses immune checkpoint blockade, including combining chemotherapy, molecularly targeted therapy, or radiotherapy, may rates outcomes. In review, we provide short background on explore different types strategies are currently being evaluated TNBC. Additionally, review why combination be beneficial, overview strategies, discuss novel immunotherapeutic opportunities approved near future
Language: Английский
Citations
2
Frontiers in Oncology, Journal Year: 2024, Volume and Issue: 14
Published: Dec. 18, 2024
Triple-negative breast cancer (TNBC) is a highly aggressive and clinically challenging subtype of cancer, lacking the expression estrogen receptor (ER), progesterone (PR), HER2/neu. The absence these receptors limits therapeutic options necessitating exploration novel treatment strategies. Epigenetic modifications, which include DNA methylation, histone microRNA (miRNA) regulation, play pivotal role in TNBC pathogenesis represent promising targets. This review delves into potential epigenetic interventions TNBC, with focus on miRNA therapeutics. We examine methylation gene silencing within development inhibitors designed to reactivate silenced tumor suppressor genes. Histone through deacetylation acetylation particular, are critical regulating expression. explore efficacy deacetylase (HDACi), have shown promise reversing aberrant patterns, thereby restoring normal function, suppressing growth. Furthermore, highlights dual miRNAs as both oncogenes suppressors discusses mimics modulating regulatory molecules inhibit progression. By integrating therapies, we propose multifaceted approach target underlying mechanisms that drive synergistic use inhibitors, HDACi, miRNA-based therapies offers avenue for personalized strategies, aiming enhance clinical outcome patients TNBC.
Language: Английский
Citations
2