Results 121 to 130 of about 41,746 (257)

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

Small-molecule inhibitors of P-Rex guanine-nucleotide exchange factors. [PDF]

Small GTPases, 2022
Lawson CD, Hornigold K, Pan D, Niewczas I, Andrews S, Clark J, Welch H.   +6 more
europepmc   +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

Identification of Rac guanine nucleotide exchange factors promoting Lgl1 phosphorylation in glioblastoma. [PDF]

J Biol Chem, 2021
Lavictoire SJ, Jomaa D, Gont A, Jardine K, Cook DP, Lorimer IAJ.   +5 more
europepmc   +1 more source

Development and analytical validation of a targeted short‐read next generation sequencing‐based pharmacogenetic panel for comprehensive variant detection

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Genomic profiling of patients for genetic variants that modify the effect of specific medications has many benefits, including the possibility of avoiding toxicities and ensuring an adequate effect of the medication. Our intention was to develop a comprehensive, high‐quality pharmacogenetic test panel for clinical use ...
Anna Gréen, Nils Johan Fredriksson, Michael Andresen, Jon Jonasson, Malin Lindqvist Appell, Henrik Gréen   +5 more
wiley   +1 more source

Role of Rho guanine nucleotide exchange factors in non-small cell lung cancer. [PDF]

Bioengineered, 2021
Zeng RJ, Xie WJ, Zheng CW, Chen WX, Wang SM, Li Z, Cheng CB, Zou HY, Xu LY, Li EM.   +9 more
europepmc   +1 more source

The Dock Family of Atypical Guanine Nucleotide Exchange Factors: Regulation by ELMO1 and RhoG

, 2008
The Dock family of proteins regulates diverse biological processes including cell migration, phagocytosis and neuronal polarization. These proteins contain a unique type of guanine nucleotide exchange factor (GEF) domain, and function as GEFs for Rho ...
Holley, Cynthia
core   +1 more source

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

British 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, Mérone Da Costa Oliveira, Adrien Levesque, Alexandre Rutault, Patrick Savoyaud, Nicolas Bréchot, Stéphane Germain   +6 more
wiley   +1 more source

The biochemical mechanism of Rho GTPase membrane binding, activation and retention in activity patterning

The EMBO Journal
Rho GTPases form plasma membrane-associated patterns that control the cytoskeleton during cell division, morphogenesis, migration, and wound repair.
Michael C Armstrong, Yannic R Weiß, Lila E Hoachlander-Hobby, Ankit A Roy, Ilaria Visco, Alison Moe, Adriana E Golding, Scott D Hansen, William M Bement, Peter Bieling   +9 more
doaj   +1 more source

Refining the treatment of immune checkpoint inhibitor–associated myocarditis: Challenges, innovations and rechallenge considerations

British Journal of Pharmacology, EarlyView.
Immune checkpoint inhibitor (ICI)‐associated myocarditis has emerged as a severe and clinically complex immune‐related toxicity that poses significant challenges for therapeutic decision‐making in routine cardio‐oncological care. High‐dose corticosteroids remain the first‐line therapy, yet their timing, dosage and tapering require careful clinical ...
Raluca I. Mincu, Lisa Zimmer, Dimitra Vlachopoulou, Elias Haj‐Yehia, Julia Hoffmann, Lars Michel, Elisabeth Livingstone, Dirk Schadendorf, Alpaslan Tasdogan, Matthias Totzeck, Tienush Rassaf   +10 more
wiley   +1 more source