Results 201 to 210 of about 3,750,504 (279)

The Histidine 382 Residue Influences the Thermal Stability and Binding Propensity of the E2 Domain of Amyloid Precursor Protein

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT The E2 domain of amyloid precursor protein (APP_E2) plays a central role in the protein's function. We reinvestigate how the missense mutation, ΔH382L, affects the domain's thermal stability and ligand binding propensity through differential scanning fluorometry.
Sphamandla Ndlovu, Candice Ngubane, Zamaxasibe Nxele, Raymond Hewer, Alexandré Delport   +4 more
wiley   +1 more source

Temporal Hydrogen‐Bond Network Analysis Reveals Substrate‐Directed Connectivity in Dihydrofolate Reductase

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT Hydrogen‐bond networks are central to protein function, but most network analyses rely on static representations that neglect how interactions evolve in time. Here, we introduce a framework that combines instantaneous and temporal graph analysis of hydrogen‐bond networks derived from molecular dynamics (MD) trajectories to quantify ligand ...
Tandac F. Guclu, Canan Atilgan, Ali Rana Atilgan   +2 more
wiley   +1 more source

Basmisanil, an α5-GABA_AR negative allosteric modulator, produces rapid and sustained antidepressant-like responses in male mice. [PDF]

Neurosci Lett
Daher F, Villalobos NA, Hanley M, Atack JR, Popa MO, Fogaça MV.   +5 more
europepmc   +1 more source

The continuing significance of chiral agrochemicals

Pest Management Science, Volume 81, Issue 4, Page 1697-1716, April 2025.
In the time frame 2018–2023, around 43% of the 35 chiral agrochemicals introduced to the market (herbicides, fungicides, insecticides, acaricides, and nematicides) contain one or more stereogenic centers in the molecule, and almost 69% of them have been marketed as racemic mixtures of enantiomers or stereoisomers.
Peter Jeschke
wiley   +1 more source

The CB1 negative allosteric modulator PSNCBAM-1 reduces ethanol self-administration via a nonspecific hypophagic effect. [PDF]

Pharmacol Biochem Behav
Buechler HM, Sumi M, Madhuranthakam IM, Donegan C, DiGiorgio F, Acosta AA, Uribe S, Rahman MA, Sorbello A, Fischer BD, Keck TM.   +10 more
europepmc   +1 more source

The metabotropic glutamate receptor 5 negative allosteric modulator fenobam: pharmacokinetics, side effects, and analgesic effects in healthy human subjects. [PDF]

Pain, 2020
Cavallone LF, Montana MC, Frey K, Kallogjeri D, Wages JM, Rodebaugh TL, Doshi T, Kharasch ED, Gereau RW.   +8 more
europepmc   +1 more source

Photo‐Switched Catalytic Amyloids

Small, EarlyView.
Photo‐switched reversible hierarchical assembly of catalytic amyloid fibrils is accomplished by mixing an amphiphilic cross‐ß peptide with a merocyanine photo switch. The peptide monomers, comprising phenylalanine‐lysine repeats, do not self‐assemble in water because of the electrostatic repulsion.
Shubhra Kanti Bhaumik, Sisira Mambram Kunnath, Elad Arad, Einat Nativ‐Roth, Arunavo Chatterjee, Albert Batushansky, Nitzan Shauloff, Hanna Rapaport, Raz Jelinek   +8 more
wiley   +1 more source

Evolutionary Mechanisms of Coagulation Factors in Cetaceans During Aquatic Adaptation

Integrative Zoology, EarlyView.
Compared with Bos taurus, T. truncatus showed shorter prothrombin time and thrombin time but prolonged activated partial thromboplastin time, indicating pathway‐specific remodeling of coagulation. Evolutionary analyses identified 18 positively selected genes and accelerated F11 evolution, while functional assays revealed increased coagulation factor ...
Wenjun Lv, Wanfei Deng, Fei Deng, Shixia Xu, Wenhua Ren   +4 more
wiley   +1 more source

Depression-like effects induced by chronic unpredictable mild stress in mice are rapidly reversed by a partial negative allosteric modulator of mGlu₅ receptor, M-5MPEP. [PDF]

Psychopharmacology (Berl)
Pałucha-Poniewiera A, Bobula B, Rafało-Ulińska A, Kaczorowska K.   +3 more
europepmc   +1 more source

Compartmentalisation in cAMP signalling: A phase separation perspective

British Journal of Pharmacology, EarlyView.
Cells rely on precise spatiotemporal control of signalling pathways to ensure functional specificity. The compartmentalisation of cyclic AMP (cAMP) and protein kinase A (PKA) signalling enables distinct cellular responses within a crowded cytoplasmic space.
Milda Folkmanaite, Manuela Zaccolo
wiley   +1 more source