The signature of extracellular vesicles in hypoxic breast cancer and their therapeutic engineering DOI Creative Commons
Beiqing Zhu,

Kehao Xiang,

Tanghua Li

et al.

Cell Communication and Signaling, Journal Year: 2024, Volume and Issue: 22(1)

Published: Oct. 21, 2024

Abstract Breast cancer (BC) currently ranks second in the global incidence rate. Hypoxia is a common phenomenon BC. Under hypoxic conditions, cells tumor microenvironment (TME) secrete numerous extracellular vesicles (EVs) to achieve intercellular communication and alter metabolism of primary metastatic tumors that shape TME. In addition, emerging studies have indicated hypoxia can promote resistance treatment. Engineered EVs are expected become carriers for treatment due their high biocompatibility, low immunogenicity, drug delivery efficiency, ease modification. this review, we summarize mechanisms TME distant metastasis BC under conditions. Additionally, highlight potential applications engineered mitigating malignant phenotypes hypoxia.

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
Toward structure–multiple activity relationships (SMARts) using computational approaches: A polypharmacological perspective DOI
Edgar López‐López, José L. Medina‐Franco

Drug Discovery Today, Journal Year: 2024, Volume and Issue: 29(7), P. 104046 - 104046

Published: May 27, 2024

Language: Английский

Citations

6
Synthesis of Novel Cyano-Acetic Acid Hydrazide Derivatives as precursor for Generation of Dihydropyridine and Pyrrole as Anticancer Agents: Multi-Target Recognition, In Vitro and In Silico Studies DOI
Sami A. Al‐Hussain,

Aya S. Saleh,

Shimaa M. Abd El‐Gilil

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141501 - 141501

Published: Jan. 1, 2025

Language: Английский

Citations

0
X-ray crystallographic and kinetic studies of biguanide containing aryl sulfonamides as Carbonic anhydrase inhibitors DOI Creative Commons
Chiara Baroni, Murat Bozdağ, Gioele Renzi

et al.

RSC Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

Dual-targeting carbonic anhydrase (CA) inhibitors bearing the biguanide group of metformin showed good selectivity against cancer related CA IX and XII. The X-ray structures two selected inhibitor complexes with hCA II XII were solved.

Language: Английский

Citations

0
The potential of Dayak tribal herbal leaves as an anti-breast cancer agent: In silico approach DOI Creative Commons

Volta Kellik Setiawan,

Ahmad Affan Ali Murtadlo, Arif Nur Muhammad Ansori

et al.

BIO Web of Conferences, Journal Year: 2025, Volume and Issue: 153, P. 01006 - 01006

Published: Jan. 1, 2025

Breast cancer is one of the leading causes mortality among women worldwide, prompting exploration alternative, natural therapies. This study examines anti-breast potential traditional herbal plants used by Dayak tribe, particularly Kleinhovia hospita Linn. Through in silico approaches, investigates cytotoxic effects and binding affinities key compounds, such as Scopoletin, Quercetin, Eleutherol, with breast cancer-related proteins. Molecular docking analysis demonstrated that Quercetin Eleutherol exhibit high (−9 −8 kcal/mol, respectively) target proteins, indicating significant for inhibiting cell proliferation targeting proteins like EGFR, JNK, NUDT5. The drug-likeness confirmed meet criteria further therapeutic exploration. These findings suggest compounds from tribal could be viable anti-cancer agents, providing a scientific foundation developing culturally relevant effective treatments cancer. Further research recommended to isolate evaluate bioactive preclinical clinical settings. work supports medicine strategy against

Language: Английский

Citations

0
Molecular Docking Appraisal of Pleurotus ostreatus Phytochemicals as Potential Inhibitors of PI3K/Akt Pathway for Breast Cancer Treatment DOI Creative Commons
Magdalene Eno Effiong, Mercy Bella-Omunagbe, Israel Sunmola Afolabi

et al.

Bioinformatics and Biology Insights, Journal Year: 2025, Volume and Issue: 19

Published: Jan. 1, 2025

Introduction: Breast cancer (BC) is a heterogeneous disease involving network of numerous extracellular signal transduction pathways. The phosphoinositide 3-kinase (PI3K)/serine/threonine kinase (Akt)/mechanistic target rapamycin (mTOR) pathway crucial for understanding the BC development. Phosphoinositide 3-kinase, phosphatase and tensin homolog (PTEN), mTOR, Akt, 3-phosphoinositide-dependent 1 (PDK1), FoxO1, glycogen synthase 3 (GSK-3), mouse double minute 2 (MDM2), H-Ras, proapoptotic B-cell lymphoma (BCL-2) family protein (BAD) proteins are key drivers this potential therapeutic targets. Pleurotus ostreatus an edible mushroom that rich in flavonoids phenols can serve as inhibitors PI3K/Akt/mTOR pathway. Aim: This study evaluated anticancer properties P through structure-based virtual screening 22 biologically active compounds present mushroom. Method: Model optimization was carried out on PI3K, PTEN, PDK1, GSK-3, MDM2, BAD molecular docking compounds/control binding pocket were simulated AutoDock Vina PyRx. drug likeness, pharmacokinetic, pharmacodynamic features prospective leads all anticipated. Result: Several potent selected driver identified from ostreatus. Ellagic acid with affinities −8.0, −8.1, −8.2, −6.2, −7.1 kcal/mol BAD, respectively, had better affinity compared their reference drugs. Likewise, apigenin (−7.8 kcal/mol), chrysin quercetin (−6.4 chlorogenic (−6.2 kcal/mol) to H-Ras proteins, respectively. Conclusion: acid, apigenin, luteolin, quercetin, chrysin, naringenin phytochemicals seen lead molecules due ability strongly bind under Analogs these also be designed

Language: Английский

Citations

0
In silico Repurposing of FDA-Approved Drugs as Multi-target Inhibitors of Glioblastoma DOI Creative Commons
Ridwan Abiodun Salaam, Funmilayo I. D. Afolayan,

Damilare Adebayo Olaniyi

et al.

Scientific African, Journal Year: 2025, Volume and Issue: unknown, P. e02582 - e02582

Published: Feb. 1, 2025

Language: Английский

Citations

0
JBI-802: the first orally available LSD1/HDAC6 dual inhibitor to enter clinical trials DOI
Jingya Zhang,

Xiangli Ren,

Yihui Song

et al.

Expert Opinion on Therapeutic Patents, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 17, 2025

Introduction Lysine-specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6) are key epigenetic regulators involved in demethylation deacetylation, processes that impact chromatin structure gene expression. JBI-802 marks a major advancement as the first novel, orally available LSD1/HDAC6 dual inhibitor currently clinical trials.

Language: Английский

Citations

0
Recent advances on anticancer activity of benzodiazine heterocycles through kinase inhibition DOI Creative Commons
Mohamed S. Nafie, Sherif Ashraf Fahmy,

Shaima H. Kahwash

et al.

RSC Advances, Journal Year: 2025, Volume and Issue: 15(7), P. 5597 - 5638

Published: Jan. 1, 2025

This is an updated review for the anticancer activity of benzodiazine heterocyclic derivatives through kinase inhibition.

Language: Английский

Citations

0
Computational Design and Synthesis of Phthalimide Derivatives as TGF-β Pathway Inhibitors for Cancer Therapeutics DOI Creative Commons
Héctor Mario Heras Martinez, Blanca Sánchez‐Ramírez, Linda-Lucila Landeros-Martínez

et al.

Chemistry, Journal Year: 2025, Volume and Issue: 7(2), P. 31 - 31

Published: Feb. 26, 2025

Background: This study investigates the synthesis and pharmacological potential of N-substituted isoindoline-1,3-dione (phthalimide) derivatives. Using M06 meta-GGA hybrid functional with a polarized 6-311G(d,p) basis set, computational evaluations assessed their impact on apoptosis modulation in colon cancer cells. Molecular docking studies targeted TGF-β protein (PDB: 1RW8) at ALK5 binding site. On this fourteen molecules were evaluated (P1–P14) six (P1, P3, P4, P5, P7, P13) demonstrated promising values. Methods: from studied compounds five (P2, P10, P11) successfully synthesized fully characterized. The reactions monitored via TLC HPLC confirming high-purity compounds. Functional groups identified through FTIR structural characterization was supported by NMR analyses. Results: Density theory calculations simulations allowed to classified as inhibitors. Synthesized derivatives developed yields 85 99% showed better affinities than Capecitabine (−6.95 kcal/mol) used control compound, P7 (5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl 2-(1,3-dioxoisoindolin-2-yl) acetate) leading group energy −12.28 kcal/mol. Other also exhibited significant affinities: P4 (−11.42 kcal/mol), P10 (−8.99 P11 (−7.50 P2 (−7.22 kcal/mol). Conclusions: Integrating insights experimental validation highlights therapeutic phthalimide derivatives, particularly P7. underscores rigorous approach identifying candidates for anticancer therapeutics, warranting further exploration.

Language: Английский

Citations

0