Results 231 to 240 of about 504,672 (298)

Bioactive Secondary Metabolites at the Ends of the Earth (2015-2025): Insights into Arctic and Antarctic Aquatic Sources. [PDF]

Mar Drugs
Phi KH, Heo EJ, Kwon S, Youn UJ, Lee S.
europepmc   +1 more source

NUAK2 Inhibition Enhances Macromolecular Drug Delivery in a 3D Fibrotic Model of the Pancreatic Tumor Microenvironment

Advanced NanoBiomed Research, EarlyView.
Using a 3D cell culture model of the fibrotic barrier in pancreatic cancer, this work shows that inhibiting NUAK2 kinase in pancreatic stellate cells enhances macromolecular drug delivery. Mechanistically, NUAK2 inhibition disrupted actin stress fiber assembly to downregulate collagen I expression, thus enhancing macromolecular permeability.
Misaki Nakamura, Hiroyoshi Y. Tanaka, Mayu Ohira, Haruko Ohta‐Okano, Reika Nakamura, Yu Seno, Saaya Yara, Sakura Fujita, Daichi Shibata, Masaya Yamamoto, Shinichi Toyooka, Kensuke Osada, Horacio Cabral, Atsushi Masamune, Mitsunobu R. Kano   +14 more
wiley   +1 more source

Design, Synthesis, and Biological Evaluation of Selective CDK4/9 Inhibitors. [PDF]

ACS Med Chem Lett
Li S, Yang X, Yin W, Zhang W, Li Z, Hu J, Li Y.   +6 more
europepmc   +1 more source

Heterogenous Model of Temozolomide Resistance in Glioblastoma Reveals Phenotypic Shifts in Drug Response and Migratory Potential

Advanced NanoBiomed Research, EarlyView.
Glioblastoma mortality is driven by cell invasion and therapeutic resistance. We report a cancer engineering approach to evaluate the behavior of heterogeneous cohorts of temozolomide resistant and responsive GBM cells. We show the effect of physiologically‐relevant metronomic dosing on ensemble drug response and invasion.
Victoria A. Kriuchkovskaia, Ela K. Eames, Sydney A. McKee, Paul J. Hergenrother, Rebecca B. Riggins, Brendan A. C. Harley   +5 more
wiley   +1 more source

The Far Side of Carboranes: Anticancer Active Monocations and Ambiently Stable Dications

Angewandte Chemie, EarlyView.
This work describes the synthesis of bench‐stable dicationic carboranes. Their enhanced electrophilicity is documented by opening the clusters with weak nucleophiles or dihydrogen. The surprising stability of positively charged carboranes in water enabled a study of their in vitro antiproliferative activity, which surpassed the effects of doxorubicin ...
Vlastimil Němec, Josef Holub, Maksim A. Samsonov, Zdeňka Růžičková, Josef Cvačka, Ján Vančo, Zdeněk Trávníček, Jan Belza, Zdeněk Dvořák, Jan Vrána, Aleš Růžička   +10 more
wiley   +2 more sources

Overcoming Regorafenib Resistance in Colorectal Cancer: Synergistic Efficacy of Cilengitide in HT29 and WiDr Cells. [PDF]

Medeni Med J
Boz AB, Semiz Z, Yanar F.
europepmc   +1 more source

Mesoporous Silica Nanoparticles With Customized Drug Ratio/Loading for Effective Treatment of Gemcitabine‐Resistant Pancreatic Tumors

Advanced NanoBiomed Research, EarlyView.
Redox responsive mesoporous silica nanoparticles (MSNs) were engineered to deliver gemcitabine (Gem) and cisplatin (cisPt) at defined ratios to overcome chemoresistance in pancreatic ductal adenocarcinoma (PDAC). Optimized Gem MSNs and Gem cisPt MSNs enhanced cytotoxicity in murine and human Gem resistant models, with select formulations inducing ...
Tamanna Binte Huq, Sudip Kumar Dam, Doaha Awad, Punnya Anil Kumar Jeeja, Farzana Ferdous, Juan L. Vivero‐Escoto   +5 more
wiley   +1 more source

Convergent Total Synthesis of 16β‐Hydroxylpseudobufarenogin

Angewandte Chemie, EarlyView.
We present a novel convergent strategy that integrates Pd/Ag‐promoted Suzuki–Miyaura coupling with Ir‐catalyzed radical‐relay cyclization, enabling the first total synthesis of 16β‐hydroxylpseudobufarenogin. This approach is broadly applicable to the total synthesis of various oxygenated bufadienolides by simply modifying the fragment structures ...
Wataru Shigematsu, Yo Matsumoto, Koichi Hagiwara, Masayuki Inoue   +3 more
wiley   +2 more sources

Cellular Target Engagement and Dissociation Kinetics of Class I-Selective Histone Deacetylase (HDAC) Inhibitors. [PDF]

Int J Mol Sci
Honin I, Novakova Z, Feller F, Schneider S, Schäker-Hübner L, Barinka C, K Hansen F.   +6 more
europepmc   +1 more source