Results 1 to 10 of about 7,182,372 (402)

Structure Activity Relationship Studies around DB18, a Potent and Selective Inhibitor of CLK Kinases

Molecules, 2022
Three series of our lead CLK1 inhibitor DB18 have been designed, synthetized and tested against CLKs and DYRK1A kinases. Their cytotoxicity was subsequently measured on seven representative cancer cell lines.
Dabbugoddu Brahmaiah, Anagani Kanaka Durga Bhavani, Pasula Aparna, Nangunoori Sampath Kumar, Hélène Solhi, Rémy Le Guevel, Blandine Baratte, Thomas Robert, Sandrine Ruchaud, Stéphane Bach, Surender Singh Jadav, Chada Raji Reddy, Paul Mosset, Nicolas Gouault, Nicolas Levoin, René Grée   +15 more
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Experimental study on inhibition of coal spontaneous combustion by hydroxyethylene diphosphonic acid

Meikuang Anquan, 2022
In order to study the effect of hydroxyethylene diphosphonic acid（HEDP） on the characteristics of coal spontaneous combustion, a temperature-programmed gas chromatography experiment was carried out to compare and analyze the production and development of
SUN Meng, WANG Fusheng, WANG Jiantao, ZHANG Chaoyang   +3 more
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The selective inhibition of the Syk tyrosine kinase ameliorates experimental autoimmune arthritis

Frontiers in Immunology, 2023
Autoimmune arthritis – such as rheumatoid arthritis – affect a significant proportion of the population, which can cause everyday joint pain, decreased mobility and reduced quality of life.
Eszter Káposztás, Eszter Káposztás, Lili Balogh, Lili Balogh, Attila Mócsai, Attila Mócsai, Éva Kemecsei, Zoltán Jakus, Tamás Németh, Tamás Németh, Tamás Németh, Tamás Németh   +11 more
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Digital Holography Study of the Inhibitory Effects of Polyaspartic Acid on the Anodic Dissolution of Inconel® 600

Electrochemistry, 2021
Electrochemical methods were used in conjunction with digital holography to study the effects of an environmentally friendly inhibitor, polyaspartic acid (PASP), on the anodic dissolution of Inconel® 600 in a 0.04 M HCl solution.
Yu SHAO, Jiaojiao QI, Boyu YUAN, Liang LI, Chao WANG   +4 more
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Development of a CDK10/CycM in vitro Kinase Screening Assay and Identification of First Small-Molecule Inhibitors

Frontiers in Chemistry, 2020
Cyclin-dependent kinases (CDKs) constitute a family of 20 serine/threonine protein kinases that play pivotal roles in the regulation of numerous important molecular and cellular processes. CDKs have long been considered promising therapeutic targets in a
Thomas Robert, Thomas Robert, Jared L. Johnson, Roxane Guichaoua, Tomer M. Yaron, Stéphane Bach, Stéphane Bach, Lewis C. Cantley, Pierre Colas   +8 more
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A novel autophagy inhibitor, bTBT, disturbs autophagosome formation

Autophagy Reports, 2023
Macroautophagy (hereafter, autophagy) is a form of intracellular degradation in which autophagosome formation is systematically coordinated by multiple processes involving numerous autophagy-related gene (ATG) proteins. Autophagy-modulating compounds are
Momoka Chiba, Mai Yanagawa, Yurika Oyama, Shingo Harada, Tetsuhiro Nemoto, Akira Matsuura, Eisuke Itakura   +6 more
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Discovery of novel spike/ACE2 inhibitory macrocycles using in silico reinforcement learning

Frontiers in Drug Discovery, 2022
Introduction: The COVID-19 pandemic has cast a heavy toll in human lives and global economics. COVID-19 is caused by the SARS-CoV-2 virus, which infects cells via its spike protein binding human ACE2.Methods: To discover potential inhibitory ...
Lev Shapira, Shaul Lerner, Guila Assayag, Alexandra Vardi, Dikla Haham, Gideon Bar, Vicky Fidelsky Kozokaro, Maayan Elias Robicsek, Immanuel Lerner, Amit Michaeli   +9 more
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Characterization and translational development of IOA-289, a novel autotaxin inhibitor for the treatment of solid tumors

Immuno-Oncology and Technology, 2023
Background: Autotaxin-lysophosphatidic acid (ATX-LPA) signaling has a predominant role in immunological and fibrotic processes, including cancer. Several ATX inhibitors and LPA receptor antagonists have been clinically evaluated, but none in patients ...
M.A. Deken, K. Niewola-Staszkowska, O. Peyruchaud, N. Mikulčić, M. Antolić, P. Shah, A. Cheasty, A. Tagliavini, A. Nizzardo, M. Pergher, L. Ziviani, S. Milleri, C. Pickering, M. Lahn, L. van der Veen, G. Di Conza, Z. Johnson   +16 more
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Extracts from European Propolises as Potent Tyrosinase Inhibitors

Molecules, 2022
Tyrosinase is a key enzyme in the melanogenesis pathway. Melanin, the product of this process, is the main pigment of the human skin and a major protection factor against harmful ultraviolet radiation (UVR).
Jarosław Widelski, Katarzyna Gaweł-Bęben, Karolina Czech, Emil Paluch, Olga Bortkiewicz, Solomiia Kozachok, Tomasz Mroczek, Piotr Okińczyc   +7 more
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DPP8 Selective Inhibitor Tominostat as a Novel and Broad-Spectrum Anticancer Agent against Hematological Malignancies

Cells, 2023
DPP8/9 inhibition induces either pyroptotic or apoptotic cell death in hematological malignancies. We previously reported that treatment with the DPP8/9 inhibitor 1G244 resulted in apoptotic cell death in myeloma, and our current study further evaluates ...
Shohei Kikuchi, Akinori Wada, Yusuke Kamihara, Kosuke Okazaki, Paras Jawaid, Mati Ur Rehman, Eiji Kobayashi, Takeshi Susukida, Tomoki Minemura, Yoshimi Nabe, Noriaki Iwao, Tatsuhiko Ozawa, Ryo Hatano, Mitsugu Yamada, Hiroyuki Kishi, Yuji Matsuya, Mineyuki Mizuguchi, Yoshihiro Hayakawa, Nam H. Dang, Yasumitsu Sakamoto, Chikao Morimoto, Tsutomu Sato   +21 more
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