Results 211 to 220 of about 87,731 (343)

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

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Muscle RING-finger proteins (MuRF) regulate protein kinase A activity via retrograde vesicular transport of PKA RI-alpha [PDF]

Nan Li, Elke Hammer, Yan Li, Uwe Voelker, Jens Fielitz   +4 more
openalex   +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

Phosphodiesterase-4 influences the PKA phosphorylation status and membrane translocation of G-protein receptor kinase 2 (GRK2) in HEK-293β2 cells and cardiac myocytes

, 2006
Xiang Li, Elaine Huston, Martin J. Lynch, Miles D. Houslay, George S. Baillie   +4 more
openalex   +1 more source

Gonadotropin-Releasing Hormone and Pituitary Adenylate Cyclase-Activating Polypeptide Affect Levels of Cyclic Adenosine 3',5'-Monophosphate-Dependent Protein Kinase A (PKA) Subunits in the Clonal Gonadotrope  T3-1 Cells: Evidence for Cross-Talk between PKA and Protein Kinase C Pathways [PDF]

, 1997
G. Garrel
openalex   +1 more source

Targeting the noncatalytic activity of GSK3β modulates neuronal excitability in medium spiny neurons via Nav1.6 interactions

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh, Zahra Haghighijoo, Akanksha Gurtu, Nolan M. Dvorak, Timothy J. Baumgartner, Nana A. Goode, Jully Singh, Matteo Bernabucci, Adam T. Szafran, Michael J. Bolt, Michael A. Mancini, Natalie M. Dvorak, Marijn Lijffijt, Zhiqing Liu, Yu Xue, Alyssa K. Thomas, Alejandro Villasante‐Tezanos, Balaji Krishnan, Jia Zhou, Fernanda Laezza   +19 more
wiley   +1 more source

v-ras and protein kinase C dedifferentiate thyroid cells by down-regulating nuclear cAMP-dependent protein kinase A.

, 1992
Ras proteins are membrane-associated transducers of eternal stimuli to unknown intracellular targets. The constitutively activated v-ras oncogene induces dedifferentiation in thyroid cells.
MUSTI A.M., BONAPACE I.M., GALLO A., GOTTESMAN M.E., GARBI, CORRADO, AVVEDIMENTO, VITTORIO ENRICO, BENUSIGLIO E., CASSANO S., FELICIELLO, ANTONIO   +8 more
core  

Author response: Reciprocal regulation of ARPP-16 by PKA and MAST3 kinases provides a cAMP-regulated switch in protein phosphatase 2A inhibition

, 2017
Veronica Musante, Lu Li, Jean Kanyo, TuKiet T. Lam, Christopher M. Colangelo, Shuk Kei Cheng, A. Harrison Brody, Paul Greengard, Nicolas Le Novère, Angus C. Nairn   +9 more
openalex   +1 more source

A novel selective stabilizer of the ryanodine receptor 2 prevents stress‐induced ventricular arrhythmias without impairing cardiac function

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Aberrant activation of type 2 ryanodine receptors (RyR2) causes lethal arrhythmias, such as catecholaminergic polymorphic ventricular tachycardia (CPVT). Developing drugs that suppress RyR2 hyperactivation may be key to novel arrhythmia treatments.
Nagomi Kurebayashi, Masami Kodama, Hana Inoue, Masato Konishi, Masami Sugihara, Takashi Murayama, Ryosuke Ishida, Koichiro Ishii, Shuichi Mori, Yukari Endo, Xi Zeng, Yukiko U. Inoue, Takayoshi Inoue, Satoru Noguchi, Hajime Nishio, Eri Nakashima, Norio Suzuki, Noriko Nakaya, Ryushi Sato, Yuya Otori, Ayuna Tsutsumi, Mirei Takahashi, Takayuki Oka, Haruo Ogawa, Kayoko Kanamitsu, Hiroyuki Kusuhara, Utako Yokoyama, Junko Kurokawa, Hiroyuki Kagechika, Takashi Sakurai   +29 more
wiley   +1 more source