Results 161 to 170 of about 4,730 (218)

The nitty‐gritty of vascular permeability in cancer: targeting blood endothelium to control metastases

open access: yesBritish Journal of Pharmacology, EarlyView.
Blood vascular permeability is a hallmark of cancer and acts as an active driver of metastatic dissemination. Metastasis accounts for the vast majority of cancer deaths, yet most work has focussed on tumour‐intrinsic traits and angiogenesis, while the specific contribution of endothelial barrier regulation to intravasation and extravasation remains ...
Pierre Boucher   +6 more
wiley   +1 more source

Targeting KRAS for cancer therapy

open access: yesBritish Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia   +4 more
wiley   +1 more source

The histone deacetylase inhibitor, suberoylanilide hydroxamic acid, restores blood–brain barrier integrity in a human stem cell‐based model of ischaemic stroke

open access: yesBritish Journal of Pharmacology, EarlyView.
Ischaemic stroke is characterised by acute cerebrovascular occlusion and blood–brain barrier (BBB) breakdown. Our results indicated that the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) ameliorated the loss of BBB integrity, changed the morphology of brain endothelial cells, increased the level of basement membrane and ...
Anikó Szecskó   +14 more
wiley   +1 more source

Thermodynamic characterisation of covalent ligand binding

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman   +4 more
wiley   +1 more source

CD93—An emerging vascular target in cancer therapy

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract CD93 is a single‐pass transmembrane glycoprotein that belongs to the C‐type lectin domain group XIV family of proteins. Although it is known to be expressed in other cell types, namely, in some subsets of immune cells, CD93 is primarily expressed on endothelial cells, where it acts as a crucial regulator of angiogenesis.
Beatriz de Alves Pereira   +3 more
wiley   +1 more source

Inhibition of leucine‐rich kinase 2 (LRRK2) promotes peripheral axon regeneration via phosphorylation‐network remodelling

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose In contrast to neurons in the central nervous system, neurons in the peripheral nervous system can regenerate axons after injury via activation of a pro‐regenerative transcriptional programme. Pathogenic mutations in leucine‐rich repeat kinase 2 (LRRK2) are the most common genetic cause of Parkinson's disease, and several small ...
Eun‐Hae Jang   +11 more
wiley   +1 more source

The Interferon-Inducible GTPases

Annual Review of Cell and Developmental Biology, 2006
Mammalian cells respond to interferons (IFNs) secreted during infection by the transcriptional upregulation of as many as a thousand genes. This remarkable transition prepares cells and organisms for resistance to infection, and many IFN-regulated gene products are players in well-understood resistance programs.
Martens, Sascha, Howard, Jonathan
openaire   +3 more sources

Regulatory GTPases

Current Opinion in Structural Biology, 1995
The past year has witnessed a tremendous increase in our understanding of the structures and interactions of the GTPases. The highlights include crystal structures of G alpha subunits, as well as the first complex between a GTPase (Rap1A) and an effector molecule (c-Raf1 Ras-binding domain).
openaire   +2 more sources

GTPases

2017
GTPases (GTP hydrolases, GTP binding proteins) are a large family of enzymes that direct various cellular functions, including signal transduction, protein biosynthesis, cell division and transport of vesicles. They are molecular switches that cycle between two conformational states (Figure 1): the inactive guanosine-5'-diphosphate (GDP)-bound state ...
Stefanini, Lucia   +2 more
openaire   +2 more sources

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