• Filter By:
• Specialty
• Source
• Condition
• Cancer
• Infectious Disease
• Drug
• Training
• Management
• Procedure
• Therapy
• Vaccine
• Nutrition
• Country

Design and synthesis of multifunctional microtubule targeting agents endowed with dual pro-apoptotic and anti-autophagic efficacy
Eur J Med Chem. 2022 Mar 20;235:114274. doi: 10.1016/j.ejmech.2022.114274. Online ahead of print.ABSTRACTAutophagy is a lysosome dependent cell survival mechanism and is central to the maintenance of organismal homeostasis in both physiological and pathological situations. Targeting autophagy in cancer therapy attracted considerable attention in the past as stress-induced autophagy has been demonstrated to contribute to both drug resistance and malignant progression and recently interest in this area has re-emerged. Unlocking the therapeutic potential of autophagy modulation could be a valuable strategy for designing innov...
Source: European Journal of Medicinal Chemistry - March 28, 2022 Category: Chemistry Authors: Giuseppe Campiani Tuhina Khan Cristina Ulivieri Leopoldo Staiano Chiara Papulino Stefania Magnano Seema Nathwani Anna Ramunno Daniel Lucena-Agell Nicola Relitti Stefano Federico Luca Pozzetti Gabriele Carullo Alice Casagni Simone Brogi Francesca Vanni Pao Source Type: research

Recent Advances in Combretastatin A-4 Inspired Inhibitors of Tubulin Polymerization-An Update
This article summarizes the new molecule development efforts to reach CA-4 analogs by modifications on its pharmacophore groups, published since 2015.PMID:34986762 | DOI:10.2174/1871526522666220105114437
Source: Current Medicinal Chemistry - January 6, 2022 Category: Chemistry Authors: Sultan Nacak Baytas Source Type: research

Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR
Eur J Med Chem. 2021 Oct 5;227:113897. doi: 10.1016/j.ejmech.2021.113897. Online ahead of print.ABSTRACTMicrotubule target agents (MTAs) are widely-used clinical anti-cancer drugs for decades, but the acquired drug resistance severely restricted their application. Thioredoxin reductases (TrxR) was reported to be overexpressed in most tumors and closely related to high risk of cancer recurrence and drug resistance, making it a potential target for anticancer drug discovery. Multi-target-directed ligands (MTDLs) by a single molecule provide a logical and alternative approach to drug combinations. In this work, based on the s...
Source: European Journal of Medicinal Chemistry - October 14, 2021 Category: Chemistry Authors: Jun Yan Yuzhu Xu Xing Jin Qiaoxuan Zhang Feng Ouyang Liqiao Han Min Zhan Xingshu Li Baoxia Liang Xianzhang Huang Source Type: research

The X-ray structure of tubulysin analogue TGL in complex with tubulin and three possible routes for the development of next-generation tubulysin analogues
Biochem Biophys Res Commun. 2021 Jun 2;565:29-35. doi: 10.1016/j.bbrc.2021.05.086. Online ahead of print.ABSTRACTMicrotubule-targeting agents (MTAs) are the most commonly used anti-cancer drugs. At least fourteen microtubule inhibitors and ten antibody drug conjugates (ADCs) linking MTAs are approved by FDA for clinical use in cancer therapy. In current research, we determined the crystal structure of tubulysin analogue TGL in complex with tubulin at a high resolution (2.65 Å). In addition, we summarized all of the previously published high-resolution crystal structures of ligands in the vinca site to provide structural i...
Source: Biochemical and Biophysical Research communications - June 5, 2021 Category: Biochemistry Authors: Wenting Li Lun Tan Zhixiong Zhang Qiuqi Xia Dongsheng Lei Yuyan Li Ting Zhang Shaoxue Zeng Xiutian Sima Yanyan Wang Source Type: research

Basket Trials for Intractable Cancer
This study has made a significant impact on clinical practice in cancer patients harboring the TRK translocation, and also illustrates the potential for future advancements in drug development and clinical trials of cancers harboring rare genomic alterations (50). Second, a basket trial may allow screening for potential efficacy across multiple tumor types in order to guide more traditional, disease-specific, follow-up studies. The goal of some basket trials is to obtain an overall assessment of the drug with pooled histologies; in such trials, subsequent analyses are straightforward, and are comparable to those in standa...
Source: Frontiers in Oncology - April 11, 2019 Category: Cancer & Oncology Source Type: research