Results 201 to 210 of about 702,558 (291)

Negative allosteric modulation of mGlu7 disrupts fear memory reconsolidation and glutamatergic signaling in rat and human brain tissue. [PDF]

Mol Psychiatry
Ciobanu AC, Caseiro DM, Niu R, Triana Del Rio R, Leroux C, Stefanelli A, Nakandakare CF, Pralong E, Daniel RT, Lütjens R, van den Burg EH, Stoop R.   +11 more
europepmc   +1 more source

Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future

Medicinal Research Reviews, EarlyView.
ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley   +1 more source

Allosteric modulation of Grb2 drives ligand-dependent signal responses. [PDF]

Biol Direct
Di Felice M, Rolfi LR, Toso J, Pennacchietti V, Ventura ES, Toto A, Tramutola A, Gianni S.   +7 more
europepmc   +1 more source

Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms

Medicinal Research Reviews, EarlyView.
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino, Manuela Bartolini, Rudolf Andrys, Kamil Musilek   +3 more
wiley   +1 more source

α₅-GABA_A allosteric modulation triggers and prolongs dopamine neuronal activity via AMPA receptors. [PDF]

J Psychopharmacol
Ahmed A, El Mansari M, Blier P.
europepmc   +1 more source

Late INa as a Therapeutic Target: New Strategies, Computational Modelling, Drug Development, and Clinical Translation

Medicinal Research Reviews, EarlyView.
ABSTRACT The Nav1.5 channel, a major isoform of voltage‐gated sodium ion channel, is mainly found in ventricular cardiomyocytes, playing a key role in generating essential cardiac action potentials for normal heart rhythms. Mutations in Nav1.5 have been associated with severe heart conditions such as long QT syndrome, Brugada syndrome, cardiac ...
Arkapravo Chattopadhyay, Lynn C. Lunsonga, Peter E. Light, Khaled Barakat   +3 more
wiley   +1 more source

eATP sensing by the purinergic receptor PA2072 for allosteric modulation in intracellular c-di-GMP signaling. [PDF]

Proc Natl Acad Sci U S A
Zhang Y, Gao X, Xiao Y, Duan Y, Xiao W, Xu Y, Yang T, Zhang H, Chen C, Shi S, Su XC, Jin X, Zhao J, Yang H, Yin G, Yuan W, Wang Z, Huang W, Lin Z.   +18 more
europepmc   +1 more source

Hsp90 Inhibition on the Western Blot: N‐Terminal Versus C‐Terminal Inhibitors in Breast Cancer

Medicinal Research Reviews, EarlyView.
ABSTRACT Heat shock protein 90 (Hsp90) is an established and clinically validated anticancer target. By regulating the folding and maturation of diverse client proteins, it is indirectly involved in carcinogenesis. Key breast cancer oncogenic drivers, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2, are ...
Jaka Dernovšek, Jernej Cingl, Urša Pečar Fonović, Tihomir Tomašič   +3 more
wiley   +1 more source

Functional spectrum of USP7 pathogenic variants in Hao-Fountain syndrome: Insights into the enzyme's activity, stability, and allosteric modulation. [PDF]

Proc Natl Acad Sci U S A
Korchak EJ, Sharafi M, Jaen Maisonet I, Salazar-Chaparro A, Semenova IV, Khan H, O'Neil AL, Caro P, Schaaf CP, Buhrlage SJ, Bezsonova I.   +10 more
europepmc   +1 more source