DePARylation is essential for cell survival and thus poly(ADP-ribose) glycohydrolase (PARG) expression correlates with cytotoxicity induced by PARG inhibition, which will benefit the development of PARG inhibitors for cancer treatment.
Multifaceted properties of the water-soluble derivative of antibiotic heliomycin enable it to offer greater antitumor value than its parent compound by inhibiting the tNOX-NAD+-SIRT1 axis to induce apoptosis.
New ATP-competitive inhibitors show properties of conformation selection when complexed with the MAP kinase, ERK2, altering movements around the activation loop.
Karolina Honzejkova, Dalibor Kosek ... Tomas Obsil
Thioredoxin functions as a negative allosteric effector of ASK1 by altering the interaction between the thioredoxin-binding and tetratricopeptide repeats domains, thereby reducing access to the kinase domain's activation segment.
The intrinsic disorder of the circadian clock protein Frequency organizes binding partners, facilitates liquid–liquid phase separation, modulates Frequency phosphorylation, and derives from sequence properties conserved with homologous clock components.
Blinding the initial review of applications for Beckman Young Investigator awards reduces prestige bias, but has no impact on the success rates for different genders.
Michael P Dalton, Mary Hongying Cheng ... Jonathan A Coleman
The structure of the vesicular monoamine transporter 2 bound to Huntington’s chorea drug tetrabenazine elucidates mechanisms of inhibition and neurotransmitter transport.
Veronica Teresa Ober, George Boniface Githure ... Michael Boshart
A minimal subset of two to three residues in cyclic nucleotide binding (CNB) domains controls nucleoside vs. cyclic nucleotide specificity, repurposing PKA of certain pathogens for novel nucleoside signaling pathways or sensing.
