Results 211 to 220 of about 139,314 (301)

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

An orally bioavailable MrgprX1-positive allosteric modulator alleviates certain neuropathic pain-related behaviors in humanized mice. [PDF]

Sci Transl Med
Uniyal A, Hin N, Zhang C, Xu Q, Huang Q, Berhane I, Thomas AG, Maragakis J, Gori S, Liu J, Zheng Q, Cui X, Peng Q, Wan J, Rais R, Slusher BS, Raja SN, Dong X, Tsukamoto T, Guan Y.   +19 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

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

A neurotensin receptor type 1-derived pepducin acts as a biased allosteric modulator to regulate target receptor function. [PDF]

Acta Pharm Sin B
Brouillette RL, Lussier F, Breault É, Meneboo N, Hassanzadeh M, Tremblay V, Chartier M, Midavaine É, Ulrich L, Côté J, Blais V, Mona CE, Longpré JM, Grandbois M, Boudreault PL, Audet M, Besserer-Offroy É, Sarret P.   +17 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

The positive allosteric modulator GNE-9278 increases gating, conductance, and Ca²⁺ permeability for GluN2D-containing NMDA receptors. [PDF]

Neuropsychopharmacology
Abbott JA, Weaver MG, Liu B, Schwarz SR, Popescu GK.   +4 more
europepmc   +1 more source

The FGF/FGFR System in the Biology and Therapeutic Landscape of Pediatric CNS Tumors

Medicinal Research Reviews, EarlyView.
ABSTRACT Central nervous system (CNS) tumors are the most common solid malignancies in children, comprising a highly heterogeneous group of neoplasms defined by distinct molecular alterations and clinical behaviors. Advances in molecular genetics have underscored the relevance of specific signaling pathways in driving pediatric tumorigenesis, among ...
Serena Filiberti, Camilla Tavani, Elena Somenza, Nicolas Tassone, Antonio d'Amati, Marta Turati, Roberto Ronca   +6 more
wiley   +1 more source

RO4938581, a GABA_A-α5 negative allosteric modulator rescued behavioral and EEG phenotypes of a mouse model of Dup15q syndrome. [PDF]

Mol Psychiatry
Nakagawa R, Nani F, Hipp JF, Honer M, Knoflach F, Gasser R, Ozmen L, Tamada K, Fjeldskaar F, Takacs L, Vautheny A, Morairty SR, Saxe M, Takumi T, Hernandez MC.   +14 more
europepmc   +1 more source