Results 71 to 80 of about 913,494 (306)

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

Selective inhibition of the kinase DYRK1A by targeting its folding process

Nature Communications, 2016
Kinase inhibitors are important drugs and usually target the ATP binding pocket of kinases. Here, Kii et al.report a completely new type of kinase inhibitor that specifically targets the protein folding intermediate state, but not the mature form, of the
Isao Kii, Yuto Sumida, Toshiyasu Goto, Rie Sonamoto, Yukiko Okuno, Suguru Yoshida, Tomoe Kato-Sumida, Yuka Koike, Minako Abe, Yosuke Nonaka, Teikichi Ikura, Nobutoshi Ito, Hiroshi Shibuya, Takamitsu Hosoya, Masatoshi Hagiwara   +14 more
doaj   +1 more source

Identification of Novel Cdc7 Kinase Inhibitors as Anti-Cancer Agents that Target the Interaction with Dbf4 by the Fragment Complementation and Drug Repositioning ApproachResearch in context

EBioMedicine, 2018
Background: Cdc7-Dbf4 is a conserved serine/threonine kinase that plays an important role in initiation of DNA replication and DNA damage tolerance in eukaryotic cells.
An Ning Cheng, Yu-Kang Lo, Yi-Sheng Lin, Tswen-Kei Tang, Chun-Hua Hsu, John T.-A. Hsu, Alan Yueh-Luen Lee   +6 more
doaj   +1 more source

Structure-based design and activity modeling of novel epidermal growth factor receptor kinase inhibitors; an in silico approach

Scientific African, 2020
The development of EGFR kinase inhibitors to treat non-small cell lung cancers is an important medical necessity due to persistent development of resistance by the mutations.
Muhammad Tukur Ibrahim, Adamu Uzairu, Gideon Adamu Shallangwa, Sani Uba   +3 more
doaj   +1 more source

Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Phosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair.
Xueqin Huang, Li You, Eugenie Nepovimova, Miroslav Psotka, David Malinak, Marian Valko, Ladislav Sivak, Jan Korabecny, Zbynek Heger, Vojtech Adam, Qinghua Wu, Kamil Kuca   +11 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

Statistical and Clustering Analysis of Safety Profiles of FDA-Approved Protein Kinase Inhibitors

Applied Sciences
Protein kinases are vital regulators in cell biology, modifying protein functions through phosphorylation. Protein kinase inhibitors (PKIs), which impede these kinases’ activities, have broadened their therapeutic scope from cancer treatment to ...
Ioana Lavinia Radulian, Georgiana Nitulescu, Anca Zanfirescu, George Mihai Nitulescu   +3 more
doaj   +1 more source

Potential and limitations of PKA/ PKG inhibitors for platelet studies

Platelets, 2022
Cyclic nucleotides (cAMP and cGMP) and corresponding protein kinases, protein kinase A (PKA) and protein kinase G (PKG), are the main intracellular mediators of endothelium-derived platelet inhibitors. Pharmacological PKA/PKG inhibitors are often used to
Valentina Shpakova, Natalia Rukoyatkina, Ulrich Walter, Stepan Gambaryan   +3 more
doaj   +1 more source

Activation of AMP-activated protein kinase by metformin induces protein acetylation in prostate and ovarian cancer cells [PDF]

, 2016
AMP-activated protein kinase (AMPK) is an energy sensor and master regulator of metabolism. AMPK functions as a fuel gauge monitoring systemic and cellular energy status.
Galdieri, Luciano, Gatla, Himavanth, Vancura, Ales, Vancurova, Ivana   +3 more
core   +2 more sources

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