Results 71 to 80 of about 1,396,646 (189)

Searching for novel carbonic anhydrase inhibitors: from virtual screening to the lab bench [PDF]

, 2013
Carbonic Anhydrases (CAs) are zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide to bicarbonate both in prokaryotes and eukaryotes.
Cadoni, Roberta, Dallocchio, Roberto, Dessì, Alessandro, Ihm, Simone, Pala, Nicolino, Roggio, Anna Maria, Sechi, Mario, Supuran, Claudiu T., Weber, Rino   +8 more
core  

Allosteric MEK1/2 Inhibitor Refametinib (BAY 86-9766) in Combination with Sorafenib Exhibits Antitumor Activity in Preclinical Murine and Rat Models of Hepatocellular Carcinoma

Neoplasia: An International Journal for Oncology Research, 2013
OBJECTIVE: The objectives of the study were to evaluate the allosteric mitogen-activated protein kinase kinase (MEK) inhibitor BAY 86-9766 in monotherapy and in combination with sorafenib in orthotopic and subcutaneous hepatocellular carcinoma (HCC ...
Roberta Schmieder, Florian Puehler, Roland Neuhaus, Maria Kissel, Alex A Adjei, Jeffrey N Miner, Dominik Mumberg, Karl Ziegelbauer, Arne Scholz   +8 more
doaj   +1 more source

Recent Advances in Natural Products Derived from Marine Echinoderms and Endophytic Microbes: Chemical Insights and Therapeutic Potential

Marine Drugs
Echinoderms, a diverse group of marine invertebrates including starfish, sea urchins, and sea cucumbers, have been recognized as prolific sources of structurally diverse natural products.
Shuangyu Li, Yan Xiao, Qiang Li, Mingzhi Su, Yuewei Guo, Xin Jin   +5 more
doaj   +1 more source

Cross-organ multi-omics profiling of microbiome and metabolome along the gut–liver axis in MASH model mice induced by western diet and MC4R knockout

Gut Pathogens
Background Western diet (WD) fed Melanocortin 4 receptor-knockout (MC4R-KO) mice develop a phenotype resembling human metabolic dysfunction-associated steatohepatitis (MASH).
Mitsuharu Matsumoto, Osamu Miura, Takeo Moriya, Hitomi Ogino, Megumi Hirayama, Akira Mitsui, Takaharu Hirayama, Yukihiko Ebisuno, Manami Kaneko, Yoshinori Satomi, Yasunori Nio   +10 more
doaj   +1 more source

Pathways Across the Valley of Death: Novel Intellectual Property Strategies for Accelerated Drug Discovery [PDF]

, 2008
Drug discovery is stagnating. Government agencies, industry analysts, and industry scientists have all noted that, despite significant increases in pharmaceutical R&D funding, the production of fundamentally new drugs - particularly drugs that work on ...
Crossman, Colin, Rai, Arti K., Reichman, Jerome H., Uhlir, Paul F.   +3 more
core   +1 more source

Renogrit selectively protects against cisplatin-induced injury in human renal tubular cells and in Caenorhabditis elegans by harmonizing apoptosis and mitophagy

Scientific Reports
Cisplatin-induced nephrotoxicity restricts its clinical use against solid tumors. The present study elucidated the pharmacological effects of Renogrit, a plant-derived prescription medicine, using cisplatin-induced human renal proximal tubular (HK-2 ...
Acharya Balkrishna, Vivek Gohel, Nishit Pathak, Monali Joshi, Rani Singh, Ankita Kumari, Rishabh Dev, Anurag Varshney   +7 more
doaj   +1 more source

Concise Synthesis and Biological Evaluation of a Phorbazole Analogue-B1 Identifies a Multi-Kinase Inhibitor with Anti-AML Activity

Marine Drugs
Phorbazoles are bioactive marine alkaloids whose development is hampered by limited supply. We report a concise synthesis of the deschloro-phorbazole core via an optimized iodine-catalyzed oxazole annulation (56% yield).
Xiang Chen, Liting Zhang, Jinqi Huang, Mingzhi Su, Yuewei Guo, Xin Jin   +5 more
doaj   +1 more source

TAK-861, a potent, orally available orexin receptor 2-selective agonist, produces wakefulness in monkeys and improves narcolepsy-like phenotypes in mouse models

Scientific Reports
Narcolepsy type 1 (NT1) is associated with severe loss of orexin neurons and characterized by symptoms including excessive daytime sleepiness and cataplexy.
Kayo Mitsukawa, Michiko Terada, Ryuji Yamada, Taku Monjo, Tetsuaki Hiyoshi, Masanori Nakakariya, Yuichi Kajita, Tatsuya Ando, Tatsuki Koike, Haruhide Kimura   +9 more
doaj   +1 more source

Technological Discontinuities and the Comparative Strategic Value of New Capabilites: Evidence from the Comparison of Small- and Large-Molecule Targeted Anti-Cancer Drug Discovery [PDF]

Traditional creative destruction theories distinguish disruptions as competence-destroying or competence-enhancing to incumbents’ capabilities, with the former case resulting in incumbents’ loss of competitive advantage in in-house R&D performance (even ...
M. Lourdes Sosa
core  

Chemical and biosynthetic potential of Penicillium shentong XL-F41

Beilstein Journal of Organic Chemistry
Penicillium strains are renowned for producing diverse secondary metabolites with unique structures and promising bioactivities. Our chemical investigations, accompanied by fermentation media optimization, of a newly isolated fungus, Penicillium shentong
Ran Zou, Xin Li, Xiaochen Chen, Yue-Wei Guo, Baofu Xu   +4 more
doaj   +1 more source