Interaction of Microcolin Cyanobacterial Lipopeptides with Phosphatidylinositol Transfer Protein (PITP)—Molecular Docking Analysis DOI Creative Commons
Christian Bailly, Gérard Vergoten

Future Pharmacology, Journal Year: 2025, Volume and Issue: 5(1), P. 13 - 13

Published: March 17, 2025

Background/Objectives: Microcolins A–M are cytotoxic marine lipopeptides produced by the cyanobacterium Moorena producens, also known as Lyngbya majuscula. Recent studies have shown that two compounds in series, microcolins B and H, can form covalent complexes with phosphatidylinositol transfer proteins α β (PITPα/β) upon reaction of their α,β-unsaturated ketone group thiol a key cysteine residue PITP. These observations prompted us to compare binding all few related derivatives (VT01454 (deoxy)majusculamide D) PITP delineate structure–binding relationships. Methods: A molecular docking analysis led identification microcolin E potentially best PITPα binder followed H analog VT01454. The computational data agree well published experimental results. Results: into large cavity positions its reactive electrophilic close Cys95, enabling facile formation C-S linkage. similar bonding occur Cys94 PITPβ. Molecular models bound were compared identify structural elements chiefly implicated recognition process. Conclusions: This study provides guidance design targeting PITPα/β considered targets for cancer inflammatory pathologies.

Language: Английский

AR and YAP crosstalk: impacts on therapeutic strategies in prostate cancer DOI Creative Commons

Guansong Zheng,

Zhaojie Yan,

Junrong Zou

et al.

Frontiers in Oncology, Journal Year: 2025, Volume and Issue: 15

Published: Feb. 3, 2025

Prostate cancer ranks as one of the most common types affecting men worldwide, and its progression is shaped by a diverse array influencing factors. The AR signaling pathway plays pivotal role in pathogenesis prostate cancer. While existing anti-androgen treatments show initial efficacy, they ultimately do not succeed halting advancement to CRPC. Recent studies have identified alterations Hippo-YAP within cancer, highlighting intricate crosstalk with pathway. In this review, we examine interactions underlying mechanisms between YAP, key molecules these two pathways. regulates stability function YAP modulating transcription, translation, phosphorylation status, while exerts both promotional inhibitory regulatory effects on AR. Based findings, paper investigates their significant roles onset, progression, therapeutic resistance discusses clinical potential treatment.

Language: Английский

Citations

1
What are the essential determinants of human papillomavirus carcinogenesis? DOI Creative Commons
Karl Münger, Elizabeth White

mBio, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 4, 2024

ABSTRACT Human papillomavirus (HPV) infection is the leading viral cause of cancer. Over past several decades, research on HPVs has provided remarkable insight into human cell biology and pathology non-viral cancers. The HPV E6 E7 proteins engage host cellular to establish an environment in infected cells that conducive virus replication. They rewire signaling pathways promote proliferation, inhibit differentiation, limit death. activity “high-risk” so potent their dysregulated expression sufficient drive initiation maintenance HPV-associated Consequently, intensive efforts have aimed identify targets E7, part with idea some or all virus-host interactions would be essential cancer drivers. These identified a large number potential binding partners each oncoprotein. However, over same time period, parallel revealed relatively small genetic mutations carcinogenesis most We therefore propose high-priority goal which many are critical drivers carcinogenesis. By identifying cancer-driving it should possible better understand distinct roles other targets, perhaps life cycle, focus develop anti-cancer therapies subset for therapeutic intervention greatest impact.

Language: Английский

Citations

6
Unravelling key signaling pathways for the therapeutic targeting of non-small cell lung cancer DOI

P. Chavan,

Ruchi Pandey,

BHEEMANAGOUDA O. PATIL

et al.

European Journal of Pharmacology, Journal Year: 2025, Volume and Issue: unknown, P. 177494 - 177494

Published: March 1, 2025

Language: Английский

Citations

0
Interaction of Microcolin Cyanobacterial Lipopeptides with Phosphatidylinositol Transfer Protein (PITP)—Molecular Docking Analysis DOI Creative Commons
Christian Bailly, Gérard Vergoten

Future Pharmacology, Journal Year: 2025, Volume and Issue: 5(1), P. 13 - 13

Published: March 17, 2025

Background/Objectives: Microcolins A–M are cytotoxic marine lipopeptides produced by the cyanobacterium Moorena producens, also known as Lyngbya majuscula. Recent studies have shown that two compounds in series, microcolins B and H, can form covalent complexes with phosphatidylinositol transfer proteins α β (PITPα/β) upon reaction of their α,β-unsaturated ketone group thiol a key cysteine residue PITP. These observations prompted us to compare binding all few related derivatives (VT01454 (deoxy)majusculamide D) PITP delineate structure–binding relationships. Methods: A molecular docking analysis led identification microcolin E potentially best PITPα binder followed H analog VT01454. The computational data agree well published experimental results. Results: into large cavity positions its reactive electrophilic close Cys95, enabling facile formation C-S linkage. similar bonding occur Cys94 PITPβ. Molecular models bound were compared identify structural elements chiefly implicated recognition process. Conclusions: This study provides guidance design targeting PITPα/β considered targets for cancer inflammatory pathologies.

Language: Английский

Citations

0