Results 191 to 200 of about 104,548 (291)

Natural aminosterols inhibit NMDA receptors with low nanomolar potency

open access: yesThe FEBS Journal, EarlyView.
Misfunction of N‐methyl‐D‐aspartate (NMDA) receptors is associated with many brain disorders, making them primary targets for drug discovery. Trodusquemine and other natural aminosterols inhibit NMDA receptors with low nanomolar potency through binding to the cell membranes followed by interaction with the channels.
Giulia Fani   +9 more
wiley   +1 more source

Y12C mutation disrupts IMPDH cytoophidia and alters cancer metabolism

open access: yesThe FEBS Journal, EarlyView.
IMPDH, the rate‐limiting enzyme for de novo GTP synthesis, can form polymers and cytoophidia to enhance activity by reducing GTP inhibition. In this study, a Y12C mutation in IMPDH2 was introduced via ABEmax base‐editing in human cancer cell lines to disrupt IMPDH polymerisation.
Chia‐Chun Chang   +7 more
wiley   +1 more source

ARF6 as a Novel Activator of HIF-2α in Pulmonary Arterial Hypertension. [PDF]

open access: yesAm J Respir Cell Mol Biol
Fellows AL   +10 more
europepmc   +1 more source

Extreme multivalency and a composite short linear motif facilitate PCNA‐binding, localisation and abundance of p21 (CDKN1A)

open access: yesThe FEBS Journal, EarlyView.
Regions flanking the PCNA‐binding motif in p21 contribute to high‐affinity binding through complementary charges without specific contacts. These regions affect p21 abundance, but their exact Lys/Arg composition is unimportant for PCNA binding. Conversely, both context and Lys/Arg composition of the N‐terminal flanking region are crucial for p21 ...
Signe Simonsen   +8 more
wiley   +1 more source

In vivo and in silico models of Drosophila for Parkinson's disease

open access: yesThe FEBS Journal, EarlyView.
In vivo and in silico models of Drosophila offer valuable advantages in the generation, analysis, and interpretation of complex biological data, thereby significantly advancing our understanding of Parkinson's disease. Molecular‐level measurements and phenotypic data from Drosophila are extensively utilised in metabolic network modeling and artificial ...
Müberra Fatma Cesur   +3 more
wiley   +1 more source

Structural insights, regulation, and recent advances of RAS inhibitors in the MAPK signaling cascade: a medicinal chemistry perspective. [PDF]

open access: yesRSC Med Chem
Prajapati V   +9 more
europepmc   +1 more source

Gαs‐specific structural elements attenuate interactions with regulator of G protein signaling (RGS) proteins

open access: yesThe FEBS Journal, EarlyView.
Heterotrimeric (αβγ) G proteins are usually inactivated by regulators of G protein signaling (RGS) proteins, but Gαs is an exception. Comparative structural analysis identified unique Gαs structural elements that may interfere with RGS binding. Mutagenesis and biochemical assays showed that three residues in the Gαs GTPase domain are both necessary and
Sabreen Higazy‐Mreih   +4 more
wiley   +1 more source

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