Results 251 to 260 of about 150,776 (304)

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

Cannabinoid and adenosine A2A receptor crosstalk regulates postnatal and adult hippocampal neurogenesis

British Journal of Pharmacology, EarlyView.
Background and purpose Adult neurogenesis is a tightly regulated process affected by both cannabinoid receptors (CB1 and CB2) and adenosine 2A (A2A) receptors, both of which modulate neural progenitor cell activity. While emerging evidence suggests an interaction between these neuromodulatory systems, the extent and mechanism of their interplay in ...
Rui S. Rodrigues, Adam Armada‐Moreira, Laura Gómez‐Acero, Filipa F. Ribeiro, Francisco M. Mouro, Ana M. Sebastião, Francisco Ciruela, Ester Aso, Sara Xapelli   +8 more
wiley   +1 more source

Identification of drug repurposing candidates for the treatment of polycystic kidney disease

British Journal of Pharmacology, EarlyView.
Background and Purpose Autosomal dominant polycystic kidney disease (ADPKD) is a leading cause of end‐stage renal disease with limited treatment options. Drug repurposing offers a promising strategy to find effective treatments. Experimental Approach We identified birinapant, bardoxolone methyl and salicylic acid as repurposing candidates for ADPKD and
Alina Meyer, Paraskevi Sotiropoulou, Koussai Bouker, Dennis Svedberg, Rebekkah Hammar, Hester Bange, Per Larsson, André Mateus, Daniel R. Dietrich, Per Artursson   +9 more
wiley   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

Functional screen for subtype specificity of voltage sensor–targeted Kv7 potentiators

British Journal of Pharmacology, EarlyView.
Background and Purpose Voltage‐gated Kv7 (potassium channel subfamily Q [KCNQ]) potassium channels are powerful modulators of neuronal excitability. ICA‐069673 is a N‐aryl benzamide drug that targets the voltage‐sensing domain (VSD) of Kv7.2 with strong selectivity over Kv7.3 or Kv7.5, but the molecular basis of this selectivity remains poorly ...
Richard Kanyo, Thomas M. Hammond, Alice W. Wang, Caroline K. Wang, Varun Aggarwal, Shawn M. Lamothe, Harley T. Kurata   +6 more
wiley   +1 more source

O‐GlcNAcylation of KAT2A Enhances Bladder Cancer Proliferation by Inhibiting the KAT2A‐TRIM22 Interaction

Cancer Science, EarlyView.
Lysine acetyltransferase 2A (KAT2A) is a transcriptional coactivator and a member of the Histone Acetyltransferase (HAT) family. While altered KAT2A activity has been implicated in various cancers, its role in bladder cancer (BLCA) remains poorly understood.
Wenjie Yang, Zhaoheng Jin, Ziyi Li, Weifeng Xu, Yingjie Li, Yueqiang Peng, Jie Dong, Lin Ma, Zhigang Ji   +8 more
wiley   +1 more source

Transient Hyperparathyroidism and Severe Intrauterine Osteopenia Linked to Novel Homozygous TRPV6 Deletion

Clinical Endocrinology, EarlyView.
ABSTRACT Context Placental calcium (Ca2+) transport is essential for foetal bone mineralisation and development, as well as for Ca2+ homoeostasis. Rare mutations in transient receptor potential vanilloid (TRPV) 6 of the infant cause insufficient maternal‐foetal Ca2+ transport through the placenta.
Teodora Grigore, Quinty Leusink, Femke Latta, Bram van der Eerden, Paul de Laat, Danielle van der Kaay, Joost Hoenderop   +6 more
wiley   +1 more source

Monocytes Derived From Human Pluripotent Stem Cells Engineered for Detection of Pyrogens

Cell Proliferation, EarlyView.
In summary, we have developed a monocyte‐based reporter system using hESC‐Mono for interrogating the NF‐κB signalling axis, a central pathway governing pyrogenic responses. Our platform enables rapid and dose‐dependent detection of both endotoxins (LPS) and non‐endotoxins (LTA and Zymosan).
Jingjing Liu, Bingyu Cai, Tingting Gao, Wumei Wei, Liu Wang, Qi Zhou, Wei Li, Jie Hao, Jun Wu   +8 more
wiley   +1 more source

A noncanonical role for Jagged1 in endothelial mechanotransduction

The FEBS Journal, EarlyView.
This study reveals a noncanonical role for Jagged1 in endothelial mechanotransduction. Shear stress modulates Jagged1 expression and subcellular localization. Loss of Jagged1 attenuates mechanotransduction and reduces Src, VEGFR2, and ERK signaling. Direct mechanical stimulation of Jagged1 induces activation of these signaling pathways.
Freddy Suarez Rodriguez, Noora Virtanen, Elmeri Kiviluoto, Rob C. H. Driessen, Feihu Zhao, Carlijn V. C. Bouten, Oscar M. J. A. Stassen, Cecilia M. Sahlgren   +7 more
wiley   +1 more source

A new branch of mammalian vitamin B6 metabolism: AKR1C‐mediated conversion of pyridoxal to pyridoxine and 4‐pyridoxolactone

The FEBS Journal, EarlyView.
Pyridoxal 5′‐phosphate (PLP) homeostasis relies on salvage enzymes, yet key metabolic branches remain undefined. We identify AKR1C isozymes as previously undescribed contributors that convert pyridoxal into pyridoxine or 4‐pyridoxolactone through reductase and dehydrogenase activities.
Nayu Kito, Yasuyuki Kitaura, Kyoka Iino, Kazuya Toriumi, Hyunah Noh, Naoya Ogawa, Makoto Arai, Hisashi Hemmi, Tomokazu Ito   +8 more
wiley   +1 more source