Results 141 to 150 of about 81,307 (285)

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

GTP cycling protein (GCP): An ancient player for allosteric gatekeeping. [PDF]

mLife
Liu JL.
europepmc   +1 more source

Songorine inhibits mitophagy in chronic heart failure via the TBC1D15/Fis1/Rab7A pathway

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Songorine (SGR) is an alkaloid extracted from Aconitum carichaelii Debx. and has a demonstrated role in cardiac dysfunction. Chronic heart failure (CHF) is a severe clinical syndrome leading to functional impairment and death, primarily due to the deterioration of energy metabolism in cardiomyocytes. However, the precise
Wenxiu Liu, Xingju Zou, Yang Zheng, Chen Sun, Cheng Peng   +4 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

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

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

A PK/PD study on antihyperalgesia by an α2/3‐GABAA receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose GABAA receptors (GABAARs) are heteropentameric ion channels that control almost all CNS functions, including spinal nociception. Most GABAARs contain a γ2 subunit but differ in their α and β subunit composition. TPA023B is an α2/α3 subtype selective, non‐sedative, positive allosteric modulator (PAM) with antihyperalgesic
Elena Neumann, Mariana O. Popa, Karen T. Elvers, Misa Oyama, Daniel Ulrich, Marcus Hanley, Gui Jie Feng, Thomas Hathaway, William T. Ralvenius, Thomas Grampp, Dietmar Benke, John R. Atack, Hanns Ulrich Zeilhofer   +12 more
wiley   +1 more source

A Rab1 interactome illuminates a dual role in autophagy and membrane trafficking. [PDF]

J Cell Biol
van Vliet AR, Gillingham AK, Morgan TE, Ohashi Y, Smith TS, Abid Ali F, Munro S.   +6 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

Induced opening of conformational switch I in GTP-bound Ran GTPase. [PDF]

Protein Sci
Czigleczki J, Dudas B, Balog E.
europepmc   +1 more source