Results 231 to 240 of about 3,750,504 (279)

A guide to transcriptional cyclin‐dependent kinases in cancer

The FEBS Journal, EarlyView.
Transcriptional cyclin‐dependent‐kinases (tCDKs) facilitate gene expression by promoting RNA polymerase II (RNAPII) progression through discrete phases of the transcription cycle. Aberrant tCDK activity is detectable in different human cancers, thereby contributing to de‐regulated gene expression programs that drive oncogenic phenotypes.
Jennifer R. Devlin, Salla Kyheröinen, Ricky W. Johnstone   +2 more
wiley   +1 more source

Hypercapnia Induces Mitochondrial Adaptations and Alters Glutamine Metabolism to Drive a Distinct Metabolic Phenotype in Monocytes

Immunology &Cell Biology, EarlyView.
Elevated CO2 (hypercapnia) is a feature of serious lung diseases, for example COPD and contributes to poor patient prognosis through modulation of immune cell function. Here we employ state‐of‐the art metabolomic and isotope tracing approaches to reveal CO2‐dependent mitochondrial alterations linked to suppressed ATP, proline and glutamate levels in ...
Ben Reddan, David E. Phelan, Xiaofei Yin, Lorraine Brennan, Martina Wallace, Eoin P. Cummins   +5 more
wiley   +1 more source

Advances in Cytosolic dsRNA Sensing of Viral Infections

Immunology &Cell Biology, EarlyView.
Activation of cytosolic dsRNA sensors by viral infection generates multiple outcomes. dsRNA generated during viral infection, either of viral origin or from endogenous sources, can activate multiple cytosolic dsRNA sensors. Activation of PKR critically induces protein translation shutdown via phosphorylation of eukaryotic translation initiation factor ...
Sofia Maceratessi, Natalia G. Sampaio
wiley   +1 more source

MyD88‐Family Adaptors: Compartmentalised Signalling and Non‐Immune Functions

Immunology, EarlyView.
MyD88‐family adaptors coordinate receptor‐ and compartment‐specific innate immune signalling across plasma membrane and endosomal pathways. At the plasma membrane, TIRAP/MAL supports MyD88‐dependent signalling downstream of TLR2 and TLR4, whereas endosomal TLR7, TLR8 and TLR9 recruit MyD88 directly.
Seshu Vardhan Pothabathula, Saurabh Mishra, Pugazhendhi Kannan, Annette Bellar, Amy Attaway, Nicole Welch, Srinivasan Dasarathy   +6 more
wiley   +1 more source

The Interactions Between Acetylcholine and T‐Cells and Their Role in the Immune System: A Scoping Review

Immunology, EarlyView.
Activated T‐cells instigate signalling events leading to the activation of transcription factors, which in turn, act on the nucleus to produce cytokines. We postulate that c‐fos is one of these transcription factors which upregulates the choline acetyltransferase gene responsible for synthesising acetylcholine (ACh).
Jarita Lay, Nicholas Manolios
wiley   +1 more source

Kinetic Benefit(s) of Allosteric Receptor Blockade by Positive Allosteric Modulator Antagonists. [PDF]

ACS Pharmacol Transl Sci
Vauquellin G, Kenakin T.
europepmc   +1 more source

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Structure–Activity Relationships for Negative Allosteric mGluR5 Modulators

ChemMedChem, 2012
AbstractA series of compounds based on the mGluR5‐selective ligand 2‐methyl‐6‐(phenylethynyl)pyridine (MPEP) were designed and synthesized. The compounds were found to be either structural analogues of MPEP, substituted monomers, or dimeric analogues. All compounds retained mGluR5 selectivity with only weak or no activity at other mGluRs or iGluRs. The
Kaae, Birgitte H, Harpsøe, Kasper, Kvist, Trine, Mathiesen, Jesper M, Mølck, Christina, Gloriam, David E, Jimenez, Hermogenes N, Uberti, Michelle A, Nielsen, Søren M, Nielsen, Birgitte, Bräuner-Osborne, Hans, Sauerberg, Per, Clausen, Rasmus Prætorius, Madsen, Ulf   +13 more
openaire   +3 more sources

Negative allosteric modulation of the µ-opioid receptor

2023
Abstract The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional opioid receptor agonists cause serious adverse effects, notably addiction and respiratory depression, which have led to the present opioid overdose epidemic. µOR negative allosteric modulators (NAMs) may serve as powerful
Evan S. O’Brien, Vipin Ashok Rangari, Amal El Daibani, Shainnel O. Eans, Betsy White, Haoqing Wang, Yuki Shiimura, Kaavya Krishna Kumar, Kevin Appourchaux, Weijiao Huang, Chensong Zhang, Jesper M. Mathiesen, Tao Che, Jay P. McLaughlin, Susruta Majumdar, Brian K. Kobilka   +15 more
openaire   +1 more source

QSAR Study of Anticonvulsant Negative Allosteric Modulators of the AMPA Receptor

Journal of Medicinal Chemistry, 2004
A quantitative structure-activity relationship (QSAR) study was performed on a set of 49 negative allosteric modulators of AMPA receptor, acting as anticonvulsant agents, using multiple linear regression. The predictive ability of the resulting model was evaluated against a set of 12 compounds; the results showed good statistics in regression and ...
MACCHIARULO, Antonio, De Luca L., Costantino G., BARRECA, MARIA LETIZIA, Gitto R., PELLICCIARI, Roberto, Chimirri A.   +6 more
openaire   +5 more sources