Results 101 to 110 of about 1,830,783 (287)

Drug repurposing through joint learning on knowledge graphs and literature

, 2018
Drug repurposing is the problem of finding new uses for known drugs, and may either involve finding a new protein target or a new indication for a known mechanism.
AlShahrani, Mona, Hoehndorf, Robert
core   +1 more source

Establishment of a structure-activity relationship of the 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness [PDF]

, 2014
The compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases (PI3Ks) and mammalian target of rapamycin (mTOR) that also showed high inhibitory potency against T. brucei cultures. With an eye towards using 1 as a starting point for
Pollastri, Michael P, Smith, Terry K, Berlanga, Manuela, Luengo-Arratta, Sandra A, Rojas-Barros, Domingo I, Saldivia, Manuel, Diaz, Rosario, Gonzalez, Silvia, Seixas, João D, Manzano, Pilar, Navarro, Miguel   +10 more
core   +1 more source

Molecular Editing Reveals a Bilobalide Chemotype that Attenuates Prolyl Endopeptidase (PREP)‐Linked Neuroinflammation

Advanced Science, EarlyView.
Molecular editing of bilobalide uncovers BB56, a PREP‐engaging chemotype with enhanced anti‐inflammatory activity in microglia. Integrated CETSA‐MS, SAR, and pathway analyses link BB56 to attenuation of p38 MAPK/NF‐κB and NLRP3‐associated inflammatory signaling, highlighting bilobalide editing as a strategy for developing neuroinflammation‐modulating ...
Chanin Sillapachaiyaporn, Wenjing Wang, Yao Qin, Lili Yan, Stephan Scheeff, Xu He, Qiong Wu, Yue Lin, Jinsai Shang, Xin Ye, Jing Liu, Kailei Sun, Chun Wai Yeung, Junzhe Huang, Zhenghui Chen, Xiaodong Liu, Yiqun Geng, Shannon Wing Ngor Au, Bonaventure Y. Ip, Ho Ko, Billy Wai‐Lung Ng   +20 more
wiley   +1 more source

Autoantigen mRNA‐LNP Vaccination Drives Therapeutic Efficacy in Preclinical Models for Autoimmunity

Advanced Science, EarlyView.
Systemic and intramuscular delivery of autoantigen mRNA via lipid nanoparticles reprograms antigen‐presenting cells toward a mature, homeostatic state, driving antigen‐specific T cell exhaustion and providing therapeutic efficacy across autoimmune disease models.
Paulien Baeten, Karen Beets, Tessa Schalley, Janne Verreycken, Gayel Duran, Daphne Lintsen, Lisa Schuetz, Xue Zhong, Rinke Nieuwschepen, Melissa Schepers, Brecht Moonen, Jeroen Bogie, Jana Van Broeckhoven, Carlo Heirman, Jurgen Van den Heuvel, Bart Vanderborght, Ismael Varela, Roxanne Nouille, Lotte Jacobs, Jessica Filtjens, Sabah Kasmi, Elise Seynaeve, Veronica Mavrovouna, Jana De Vrieze, Michael A. Brehm, Sandra Maréchal, Sophie Janssens, Florence Lambolez, Niels Hellings, Stefaan De Koker, Bieke Broux   +30 more
wiley   +1 more source

Drug repurposing with network reinforcement

BMC Bioinformatics, 2019
Drug repurposing has been motivated to ameliorate low probability of success in drug discovery. For the recent decade, many in silico attempts have received primary attention as a first step to alleviate the high cost and longevity. Such study has taken benefits of abundance, variety, and easy accessibility of pharmaceutical and biomedical data ...
Yonghyun Nam, Myungjun Kim, Hang-Seok Chang, Hyunjung Shin   +3 more
openaire   +4 more sources

PDGFRα+/Integrin α2+ Fibroblasts Orchestrate Tumor Budding in Oral Squamous Cell Carcinoma via Mechano‐Metabolic Symbiosis: E‐Cadherin/Integrin α2β1 Adhesion and Mitochondrial Transfer

Advanced Science, EarlyView.
PDGFA/PDGFRα signaling recruits CAFs to OSCC nests, and CAF‐OSCC contact drives tumor budding invasion. Mechanistically, heterotypic adhesion via E‐cadherin/integrin α2β1 activates YAP signaling in OSCC cells, inducing EMT. Concurrently, CAFs transfer mitochondria through TNTs, supplying ATP to fuel invasion.
Yufang Liu, Jiao Li, Juan Liu, Qi Dong, Haoyang Zhang, Yanjin Wang, Huibing Li, Ye Guan, Lei Cao, Manqing Zhang, Fangning Guo, Xue Liu, Zhen Yang, Mengmeng Lu, Hui Liu, Laiping Zhong, Tong Ji, Tingjiao Liu   +17 more
wiley   +1 more source

Has the human biological interaction with SARS‐CoV2 variants entered a pliant “Faustian bargain”?

Pharmacology Research & Perspectives
We hypothesize that a “Faustian bargain”—the trading of increased SARS—CoV2 viral infection with a concurrent potential for prevention of life‐threatening lower lung infection explains the previous and future morbidity and mortality from COVID‐19 ...
Richard J. Head, Marko Popovic, Jennifer H. Martin   +2 more
doaj   +1 more source

bio-ontology-research-group/multi-drug-embedding: Method for drug repurposing from knowledge graphs and literature

, 2018
Method for drug repurposing from knowledge graphs and ...
AlShahrani, Mona, Hoehndorf, Robert
core   +1 more source

Penfluridol Triggers GSDME‐Mediated Immunogenic Pyroptosis to Potentiate Antitumor Immunotherapy

Advanced Science, EarlyView.
A high‐throughput screen of FDA‐approved antipsychotics identifies penfluridol as a potent pyroptosis inducer acting via direct TTI1 inhibition. This triggers TNFA‐NFKB signaling and caspase‐8/‐3‐dependent GSDME cleavage. The compound stimulates antitumor immunity alone and synergizes with anti‐PD‐1 therapy, while low TTI1 expression emerges as a ...
Linfeng Li, Daishi Li, Danyao Chen, Yating Dian, Lei Yao, Hui Su, Ziyu Guo, Deze Zhao, Zihua Wu, Furong Zeng, Chunfang Zhang, Guangtong Deng   +11 more
wiley   +1 more source

Liver Endothelia Orchestrate MASH‐Associated Macrophage Zonation Through FSTL1‐ITGA4 Axis

Advanced Science, EarlyView.
Liver inflammation in MASH fundamentally hinges on the newly defined Kit/STAT2/FSTL1/ITGA4 axis. Declining endothelial Kit collapses normal hepatic zonation, driving an aberrant FSTL1 gradient that recruits pathogenic macrophages. Strikingly, targeting FSTL1‐ITGA4 with anti‐VLA4 restores spatial immune homeostasis and halts disease progression ...
Lin Sun, Zhensheng Yue, Zhiqiang Fang, Hao Xu, Wei Du, Yuwei Ling, Jingjing Liu, Ping Song, Fei He, Juanli Duan, Lin Wang   +10 more
wiley   +1 more source