Results 151 to 160 of about 82,021 (288)

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

British Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

Rab5 nucleotide binding promotes oxidative metabolism to fuel hepatocellular carcinoma cell proliferation. [PDF]

J Biol Chem
Otakhor KO, Zaidi MAA, Oberley-Deegan RE, Ponnusamy MP, Fisher KW, Schott MB.   +5 more
europepmc   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

Mammalian evolution and human mutation burden in Rab GTPases. [PDF]

Biochem Biophys Rep
Sidor U, Hughes GM, Simpson JC.
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

Optogenetic Tools for Spatiotemporal Interrogation of Cytoskeletal Dynamics. [PDF]

Bioconjug Chem
Du DT, Price A, Lan TH, Zhou Y.
europepmc   +1 more source

Therapeutic potential of small molecules that block receptor‐induced Kv7/M‐current suppression in neuroprotection, seizures, and pain

British Journal of Pharmacology, EarlyView.
Receptor‐induced Kv7/M‐current suppression increases neuronal activity and contributes to pathology of several conditions. A new class of Kv7 modulators identified in this study attenuates M‐current suppression and shows therapeutic effects. Abstract Background and Purpose Neuronal Kv7 channels generate low voltage–gated potassium currents known as the
Young Woo Kim, Pavan Kumar Behara, Lamees Alhassen, Cindy Wong, Olivier Civelli, Naoto Hoshi   +5 more
wiley   +1 more source

Rho Small GTPase Family in Androgen-Regulated Prostate Cancer Progression and Metastasis. [PDF]

Cancers (Basel)
Hairston DWS, Mudryj M, Ghosh PM.
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

Targeting the Ras-Ral Signaling Axis in Type 2 Diabetes Mellitus: A Dual-Modulation Approach to Correcting Insulin Resistance and β-Cell Dysfunction. [PDF]

Pharmaceuticals (Basel)
Thulasi N, Harithpriya K, Ganesan K, Ramkumar KM.   +3 more
europepmc   +1 more source