Results 181 to 190 of about 3,750,504 (279)

Blocking glutamate mGlu₅ receptors with the negative allosteric modulator CTEP improves disease course in SOD1^G93A mouse model of amyotrophic lateral sclerosis. [PDF]

Br J Pharmacol, 2021
Milanese M, Bonifacino T, Torazza C, Provenzano F, Kumar M, Ravera S, Zerbo AR, Frumento G, Balbi M, Nguyen TPN, Bertola N, Ferrando S, Viale M, Profumo A, Bonanno G.   +14 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

The Pathway to Proof-of-Concept for BNC210, a Negative Allosteric Modulator of the Alpha-7 Nicotinic Acetylcholine Receptor (nAChR), for Treatment of Psychiatric Disease. [PDF]

Clin Pharmacol Drug Dev
Rolan P, Doolin E, Paul D, Crossman J, Odontiadis M, Danjou P, Smith M, Papapetropoulos S.   +7 more
europepmc   +1 more source

Optical control of pain in vivo with a photoactive mGlu receptor negative allosteric modulator

Altres ajuts: ICREA (ICREA Academia-2010), Fundació la Marató de TV3 (Grant 20152031) and IWT (SBO-140028).Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex ...
Bresolí-Obach, Roger, Font, Joan, López-Cano, Marc, Ciruela, Francisco, Llebaria, Amadeu, Scarselli, Pamela, Fernández-Dueñas, Víctor, Nonell, Santi, Goudet, Cyril, Catena, Juanlo, Malhaire, Fanny, Di Pietro, Paola, Battaglia, Giuseppe, Giraldo, Jesús, Pin, Jean-Philippe, Nicoletti, Ferdinando, Rovira, Xavier, Notartomaso, Serena   +17 more
core  

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

On-Cell Saturation Transfer Difference NMR Spectroscopy on Ion Channels: Characterizing Negative Allosteric Modulator Binding Interactions of P2X7. [PDF]

J Am Chem Soc
Monaco S, Browne J, Wallace M, Angulo J, Stokes L.   +4 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

Safety and Efficacy of the NMDA-2b-Selective Negative Allosteric Modulator BI 1569912: A Phase Ib Randomized Trial in Major Depressive Disorder. [PDF]

Clin Pharmacol Ther
McIntyre RS, Sanacora G, Walling DP, Cohen EA, Malhotra S, Rosenbrock H, Schmitz M, Scholz A, Süssmuth SD, De Crescenzo F.   +9 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