Results 41 to 50 of about 804,673 (258)

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

PXR Suppresses PPARα-Dependent HMGCS2 Gene Transcription by Inhibiting the Interaction between PPARα and PGC1α

Cells, 2021
Background: PXR is a xenobiotic-responsive nuclear receptor that controls the expression of drug-metabolizing enzymes. Drug-induced activation of PXR sometimes causes drug–drug interactions due to the induced metabolism of co-administered drugs.
Ryota Shizu, Kanako Ezaki, Takumi Sato, Ayaka Sugawara, Takuomi Hosaka, Takamitsu Sasaki, Kouichi Yoshinari   +6 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

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

Unlocking therapeutic potential: exploring cross-talk among emerging nuclear receptors to combat metabolic dysfunction in steatotic liver disease

npj Metabolic Health and Disease
Nuclear receptors (NRs) regulate cellular processes and serve as key targets in treating metabolic dysfunction-associated steatotic liver disease (MASLD) and steatohepatitis (MASH).
Milton Boaheng Antwi, Ariann Jennings, Sander Lefere, Dorien Clarisse, Anja Geerts, Lindsey Devisscher, Karolien De Bosscher   +6 more
doaj   +1 more source

Structural biology of ferritin nanocages

FEBS Letters, EarlyView.
Ferritin is a conserved iron‐storage protein that sequesters iron as a ferric mineral core within a nanocage, protecting cells from oxidative damage and maintaining iron homeostasis. This review discusses ferritin biology, structure, and function, and highlights recent cryo‐EM studies revealing mechanisms of ferritinophagy, cellular iron uptake, and ...
Eloise Mastrangelo, Flavio Di Pisa
wiley   +1 more source

Nuclear receptors in osteoclasts

Current Opinion in Pharmacology, 2020
Osteoclasts are bone-resorbing cells that play an essential role in the remodeling of bone under physiological conditions and numerous pathological conditions, such as osteoporosis, bone metastasis, and inflammatory bone erosion. Nuclear receptors are crucial to various physiological processes, including metabolism, development and inflammation, and ...
Seyeon, Bae, Steven, Zeng, Kyung-Hyun, Park-Min   +2 more
openaire   +3 more sources

Organ‐specific redox imbalances in spinal muscular atrophy mice are partially rescued by SMN antisense oligonucleotides

FEBS Letters, EarlyView.
We identified a systemic, progressive loss of protein S‐glutathionylation—detected by nonreducing western blotting—alongside dysregulation of glutathione‐cycle enzymes in both neuronal and peripheral tissues of Taiwanese SMA mice. These alterations were partially rescued by SMN antisense oligonucleotide therapy, revealing persistent redox imbalance as ...
Sofia Vrettou, Brunhilde Wirth
wiley   +1 more source

Nuclear Receptors

Science's STKE, 2005
This Teaching Resource provides lecture notes and slides for a class covering nuclear receptors and is part of the course "Cell Signaling Systems: A Course for Graduate Students." The lecture begins with a discussion of the structure of nuclear hormone receptors and then proceeds to describe mechanisms of transcriptional regulation, modulation of ...
  +5 more sources

A Convenient Laboratory‐Scale Synthesis Route Toward the PPARα Agonist Pemafibrate

ChemistryOpen
Pemafibrate is a potent and selective agonist of peroxisome proliferator‐activated receptor alpha (PPARα). It was designed to improve lipid metabolism with enhanced safety and efficacy compared to traditional fibrates and is clinically approved in Japan ...
Felien Morlion, Dorien Clarisse, Karolien De Bosscher, Matthias D’hooghe   +3 more
doaj   +1 more source