Results 61 to 70 of about 10,836 (202)

Cancer pain: current practice and emerging targets

British Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye, Marcin Chwistek, Zhiting Gong, Vanessa Uzonwanne, Xiaojie Shi, Arpad Szallasi   +5 more
wiley   +1 more source

The substance P receptor, which couples to Gq/11, is a substrate of beta-adrenergic receptor kinase 1 and 2

Journal of Biological Chemistry, 1993
The agonist-occupied forms of several G-protein-coupled receptors that modulate the activity of adenylycyclase via Gs (e.g. beta 2-adrenergic) or Gi (e.g. alpha 2-adrenergic and cardiac muscarinic) are phosphorylated by beta-adrenergic receptor kinases (beta ARK 1 and beta ARK 2).
M M, Kwatra, D A, Schwinn, J, Schreurs, J L, Blank, C M, Kim, J L, Benovic, J E, Krause, M G, Caron, R J, Lefkowitz   +8 more
openaire   +2 more sources

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

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

Endothelium‐ and epithelium‐derived novel endogenous catecholamines as modulators of the autonomic nervous system

British Journal of Pharmacology, EarlyView.
Abstract Catecholamines are classically viewed as neuronal transmitters and adrenal hormones; however, accumulating evidence demonstrates that sources other than nerve fibres and adrenal medulla play a fundamental role in local organ regulation. Physiological paradoxes, such as preserved organ function after denervation or transplantation, challenge a ...
Mariana G. de Oliveira, Edson Antunes, Fabiola Zakia Monica, Gilberto De Nucci   +3 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

Overexpression of beta-arrestin and beta-adrenergic receptor kinase augment desensitization of beta 2-adrenergic receptors.

Journal of Biological Chemistry, 1993
Receptor-specific or homologous desensitization of beta 2-adrenergic receptors is thought to be effected via phosphorylation of the receptor by the beta-adrenergic receptor kinase (beta ARK), followed by binding of beta-arrestin. We have generated stably transfected Chinese hamster ovary cell lines overexpressing either of the two regulatory proteins ...
S, Pippig, S, Andexinger, K, Daniel, M, Puzicha, M G, Caron, R J, Lefkowitz, M J, Lohse   +6 more
openaire   +2 more sources

Unveiling Gut Homeostasis Disruption in Sepsis: Towards an Integrated Mechanistic and Translational Roadmap

Cell Proliferation, EarlyView.
Elucidating the contribution of gut‐organ axes will provide new insights for developing combined therapeutic strategies against sepsis‐associated multiple organ dysfunction. ABSTRACT Sepsis, a life‐threatening clinical syndrome precipitated by a maladaptive host response to infection, is associated with substantial morbidity and high mortality rates ...
Yichen Bao, Lin Qi, Guijun Zou, Xingpeng Yang, Yizhao Ma, Zhifu Li, Xiaohui Du, Pengyue Zhao   +7 more
wiley   +1 more source

Agonist-dependent recruitment of phosphoinositide 3-kinase to the membrane by beta-adrenergic receptor kinase 1. A role in receptor sequestration.

The Journal of biological chemistry, 2001
Agonist-dependent desensitization of the beta-adrenergic receptor requires translocation and activation of the beta-adrenergic receptor kinase1 by liberated Gbetagamma subunits. Subsequent internalization of agonist-occupied receptors occurs as a result of the binding of beta-arrestin to the phosphorylated receptor followed by interaction with the AP2 ...
Naga Prasad S.V., Barak L.S., RAPACCIUOLO, ANTONIO, Caron M.G., Rockman H.A.   +4 more
openaire   +2 more sources

Spatiotemporal dynamics of β‐arrestin‐mediated Src activation in 5‐HT7 receptor signaling pathway

The FEBS Journal, EarlyView.
GPCRs induce distinct cellular responses via G protein‐ or β‐arrestin‐mediated signaling pathways. This study revealed that β‐arrestin‐biased 5‐HT7R ligand induces slow, sustained Src activation, contrasting with transient G protein‐mediated activation.
Hyunbin Kim, Yong Woo Lee, Huimin Lee, Eunseo Park, Jieon Lee, Hae Nim Lee, Kyeong‐Man Kim, Hyunah Choo, Jihye Seong   +8 more
wiley   +1 more source