Results 161 to 170 of about 219,778 (281)

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

Pharmacologic profiling of phosphoinositide 3-kinase inhibitors as mitigators of ionizing radiation-induced cell death. [PDF]

J Pharmacol Exp Ther, 2013
Lazo JS, Sharlow ER, Epperly MW, Lira A, Leimgruber S, Skoda EM, Wipf P, Greenberger JS.   +7 more
europepmc   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Dual pharmacological targeting of coactivator‐associated arginine methyltransferase 1 (CARM1) and salt inducible kinase (SIK) drives ketogenesis in both hepatocytes and mice

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Ketone bodies are liver‐derived circulating energy metabolites that positively impact most hallmarks of ageing. Ketone bodies increase during calorie restriction and fasting, two of the more widely perceived methods to increase health span.
Tábata Bergonci, Troels Kjær Rosenbæk, Samuel J. Windross, Ulrik B. Keiding, Estéfano Pinilla, Katrine P. Stuckert, Jakob Hansen, Camilla B. Nielsen, Jemila Peter Gomes, Lucy R. Davies, Johan Palmfeldt, Volker Loeschcke, Charlotte U. Andersen, Ulf Simonsen, Thomas B. Poulsen, Mogens Johannsen   +15 more
wiley   +1 more source

Cardiotoxicity of BRAF/MEK inhibitors

British Journal of Pharmacology, EarlyView.
Abstract Rapidly accelerated fibrosarcoma type B/B‐Raf proto‐oncogene, serine/threonine kinase (BRAF) and mitogen‐activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real‐world clinical practice.
Katharina Seuthe, Valerie Lohner, Kevin Terre, Thomas Riffelmacher, Roman Pfister   +4 more
wiley   +1 more source

Phosphoinositide-3-Kinase Catalytic Alpha and KRAS Mutations are Important Predictors of Resistance to Therapy with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Patients with Advanced Non-small Cell Lung Cancer

Journal of Thoracic Oncology, 2011
V. Ludovini, F. Bianconi, L. Pistola, R. Chiari, V. Minotti, R. Colella, D. Giuffrida, F. Tofanetti, A. Siggillino, A. Flacco, E. Baldelli, D. Iacono, M. Mameli, A. Cavaliere, L. Crinò   +14 more
semanticscholar   +1 more source

Impact of incretin analogues on lipid and lipoprotein metabolism in obesity and diabetes

British Journal of Pharmacology, EarlyView.
Abstract Incretin‐based therapies have gained momentum as a key strategy for reducing cardiovascular risk in individuals with obesity and/or type 2 diabetes (T2D). It remains unclear whether the cardiovascular benefits reflect a direct reduction in atherogenic lipoproteins—namely, low‐density lipoproteins (LDL), very low‐density lipoproteins (VLDL) and
Andrea Baragetti, Giuseppe Danilo Norata
wiley   +1 more source

MAPK Inhibitor‐Tolerant Persister Cells in Melanoma: Mechanisms and Therapeutic Vulnerabilities

Cancer Science, EarlyView.
Melanoma response to MAPK inhibition progresses from drug‐sensitive cells to drug‐tolerant persister states, which enable survival through adaptive signaling, metabolic rewiring, and phenotypic plasticity. These persister cells serve as an intermediate reservoir from which resistant tumors ultimately emerge. ABSTRACT Though major advancements have been
Bhoomi Shah, Mackenzie M. Mayhew, Jacob Sellers, Russell G. Witt   +3 more
wiley   +1 more source

Gasdermin‐Mediated Pyroptosis: Novel Strategies Against Colorectal Cancer

Cancer Science, EarlyView.
Pyroptosis is a double‐edged sword in colorectal cancer (CRC): chronic low‐grade pyroptosis promotes tumor progression, whereas acute induction of pyroptosis in cancer cells triggers antitumor immunity and enhances therapeutic response. Targeting gasdermin‐mediated pyroptosis represents a promising strategy for CRC treatment.
Kaibo Guo, Yuqian Feng, Jiamin Lu, Nuerbiye Abudurexiti, Xinlei Zhou, Mengfan Wei, Song Zheng   +6 more
wiley   +1 more source

Approaches to visualize, quantify, and manipulate phosphoinositides in cells. [PDF]

Histochem Cell Biol
Gönül R, Chytła A, Miladinović A, Antiga L, Hozák P, Sztacho M.   +5 more
europepmc   +1 more source