Results 141 to 150 of about 4,357,163 (359)

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

Cell density–dependent nuclear‐cytoplasmic shuttling of SETDB1 integrates with Hippo signaling to regulate YAP1‐mediated transcription

FEBS Letters, EarlyView.
At low cell density, SETDB1 and YAP1 accumulate in the nucleus. As cell density increases, the Hippo pathway is gradually activated, and SETDB1 is associated with increased YAP1 phosphorylation. At high cell density, phosphorylated YAP1 is sequestered in the cytoplasm, while SETDB1 becomes polyubiquitinated and degraded by the ubiquitin–proteasome ...
Jaemin Eom, Jaewoong Jang, Jung Sun Park, Yong‐Kook Kang   +3 more
wiley   +1 more source

KU124 (9,10,10-trioxo-N-(2-phenylphenyl)thioxanthene-3-carboxamide) as a novel inhibitor of TASK-1

Frontiers in Pharmacology
TASK-1 is a two-pore K+ leak channel. The name, TASK-1, stands for TWIK-related acid-sensitive potassium channel 1, and this channel is encoded by the KCNK3 gene.
Ana Dumani, Annette Jacob, Diego Chavez, Abena Amankwaa, Ramish Zahed, Martha Julemis, Hinaben Patel, Joana Lopez, Steven Almazan, Patrick Martins, Anthony Contreras, Sofiia Korotka, Gianna Kiszka, Alexander Aleynik, Justin Patino, David Graham, Megan Blaisdell, Youssef Elhowary, Shuayb Yousuf, Chelsea Pelley, Jenna Marciano, Jessica Best, Rhustie Valdizno, Nikki Mastrodomenico, Jonelle Brown, Sarah Schwartz, Irene Anin, Yara Farrag, Rinchu George, Gianna Medeiros, Sophia Lang, Marilyn Dennis, Oluwatoni Awoleye, Lamont Lee, Ericka Salgado, Diana Figueroa Chea, Thomas Walter Comollo, Thomas Walter Comollo   +37 more
doaj   +1 more source

Inhibiting stearoyl‐CoA desaturase suppresses bone metastatic prostate cancer by modulating cellular stress, mTOR signaling, and DNA damage response

FEBS Letters, EarlyView.
Bone metastasis in prostate cancer (PCa) patients is a clinical hurdle due to the poor understanding of the supportive bone microenvironment. Here, we identify stearoyl‐CoA desaturase (SCD) as a tumor‐promoting enzyme and potential therapeutic target in bone metastatic PCa.
Alexis Wilson, Mackenzie K Herroon, Shane Mecca, Laimar C Garmo, Jacob Lindquist, Shrila Rajendran, Steve M. Patrick, Izabela Podgorski   +7 more
wiley   +1 more source

Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals

Molecules
Cathepsin K plays a pivotal role in bone resorption and has emerged as a prominent therapeutic target for treating bone-related diseases such as osteoporosis.
Dong Oh Moon
doaj   +1 more source

Molecular dynamics based methods for the computation of standard binding free energies and binding selectivity of inhibitors of proteins of pharmaceutical interest

, 2021
Michail Papadourakis
openalex   +1 more source

The (Glg)ABCs of cyanobacteria: modelling of glycogen synthesis and functional divergence of glycogen synthases in Synechocystis sp. PCC 6803

FEBS Letters, EarlyView.
We reconstituted Synechocystis glycogen synthesis in vitro from purified enzymes and showed that two GlgA isoenzymes produce glycogen with different architectures: GlgA1 yields denser, highly branched glycogen, whereas GlgA2 synthesizes longer, less‐branched chains.
Kenric Lee, Dimitrios Bekiari, Sofia Doello, Karl Forchhammer   +3 more
wiley   +1 more source

Etoposide targets 2A protease to inhibit enterovirus 71 replication

Microbiology Spectrum
Enterovirus 71 (EV71) is a major pathogen that causes hand, foot, and mouth disease (HFMD) in infants and children. Notably, no clinically approved drugs specifically target EV71.
Qinqin Liang, Sai Shi, Qingjie Zhang, Yaxin Wang, Sheng Ye, Binghong Xu   +5 more
doaj   +1 more source

Myocarditis in Patients Treated With Immune Checkpoint Inhibitors

, 2018
Syed Mahmood, Michael G. Fradley, Justine V. Cohen, Anju Nohria, Kerry L. Reynolds, Lucie Heinzerling, Ryan J. Sullivan, Rongras Damrongwatanasuk, Carol L. Chen, Dipti Gupta, Michael Constantin Kirchberger, Magid Awadalla, Malek Hassan, Javid J. Moslehi, Sachin Shah, Sarju Ganatra, Paaladinesh Thavendiranathan, Donald P. Lawrence, John D. Groarke, Tomas G. Neilan   +19 more
openalex   +2 more sources

Angiogenesis Inhibitors [PDF]

Journal of Thoracic Oncology, 2011
Das, Millie, Wakelee, Heather
openaire   +4 more sources