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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

GRK2 expression and catalytic activity are essential for vasoconstrictor / ERK-stimulated arterial smooth muscle proliferation
Biochem Pharmacol. 2023 Sep 8:115795. doi: 10.1016/j.bcp.2023.115795. Online ahead of print.ABSTRACTProlonged vasoconstrictor signalling found in hypertension, increases arterial contraction, and alters vessel architecture by stimulating arterial smooth muscle cell (ASMC) growth, underpinning the development of re-stenosis lesions and vascular remodelling. Vasoconstrictors interact with their cognate G protein coupled receptors activating a variety of signalling pathways to promote smooth muscle proliferation. Here, angiotensin II (AngII) and endothelin 1 (ET1), but not UTP stimulates ASMC proliferation. Moreover, siRNA-me...
Source: Biochemical Pharmacology - September 10, 2023 Category: Drugs & Pharmacology Authors: Asma Alonazi Craig A Nash Chuan-Han Wang Elena Christofidou R A John Challiss Jonathon M Willets Source Type: research

Hydrogen sulfide promoted retinoic acid-related orphan receptor α transcription to alleviate diabetic cardiomyopathy
Biochem Pharmacol. 2023 Aug 15:115748. doi: 10.1016/j.bcp.2023.115748. Online ahead of print.ABSTRACTDiabetic cardiomyopathy (DCM) is one serious and common complication in diabetes without effective treatments. Hydrogen sulfide (H2S) fights against a variety of cardiovascular diseases including DCM. Retinoic acid-related orphan receptor α (RORα) has protective effects on cardiovascular system. However, whether RORα mediates the protective effect of H2S against DCM remains unknown. The present research was to explore the roles and mechanisms of RORα in H2S against DCM. The study demonstrated that H2S donor sodium hydro...
Source: Biochemical Pharmacology - August 17, 2023 Category: Drugs & Pharmacology Authors: Shuping Zhang Jieru Shen Yu Zhu Yangyang Zheng Wenqin San Danyi Cao Yun Chen Guoliang Meng Source Type: research

Curcumin protects against the age-related hearing loss by attenuating apoptosis and senescence via activating Nrf2 signaling in cochlear hair cells
This study is the first to demonstrate that curcumin can prevent oxidative stress-induced auditory hair cell degeneration through Nrf2 activation, highlighting its potential therapeutic value in preventing ARHL.PMID:37334787 | DOI:10.1016/j.bcp.2023.115575
Source: Biochemical Pharmacology - June 19, 2023 Category: Drugs & Pharmacology Authors: Ning Li Xirui Yan Weiling Huang Min Chu Yang Dong Haiyan Song Yinting Peng Jianrong Shi Qing Liu Source Type: research

VPS34-IN1 induces apoptosis of ER  + breast cancer cells via activating PERK/ATF4/CHOP pathway
Biochem Pharmacol. 2023 Jun 6:115634. doi: 10.1016/j.bcp.2023.115634. Online ahead of print.ABSTRACTVPS34-IN1 is a specific selective inhibitor of Class III Phosphatidylinositol 3-kinase (PI3K) and has been shown to exhibit a significant antitumor effect in leukemia and liver cancer. In current study, we focused on the anticancer effect and potential mechanism of VPS34-IN1 in estrogen receptor positive (ER + ) breast cancer. Our results revealed that VPS34-IN1 inhibited the viability of ER + breast cancer cells in vitro and in vivo. Flow cytometry and western blot analyses showed that VPS34-IN1 treatment induced breast can...
Source: Biochemical Pharmacology - June 8, 2023 Category: Drugs & Pharmacology Authors: Qiuya Wu Duanfang Zhou Zhengze Shen Bo Chen Gang Wang Lihong Wu Limei Zhang Xiaoli Li Lie Yuan Yuanli Wu Na Qu Weiying Zhou Source Type: research

Differential regulation of histamine H < sub > 1 < /sub > receptor-mediated ERK phosphorylation by G < sub > q < /sub > proteins and arrestins
Biochem Pharmacol. 2023 May 16:115595. doi: 10.1016/j.bcp.2023.115595. Online ahead of print.ABSTRACTGq protein-coupled histamine H1 receptors play crucial roles in allergic and inflammatory reactions, in which the phosphorylation of extracellular signal-regulated kinase (ERK) appears to mediate the production of inflammatory cytokines. ERK phosphorylation is regulated by G protein- and arrestin-mediated signal transduction pathways. Here, we aimed to explore how H1 receptor-mediated processes of ERK phosphorylation might be differentially regulated by Gq proteins and arrestins. For this purpose, we evaluated the regulator...
Source: Biochemical Pharmacology - May 18, 2023 Category: Drugs & Pharmacology Authors: Shotaro Michinaga Ayaka Nagata Ryosuke Ogami Yasuhiro Ogawa Shigeru Hishinuma Source Type: research

Targeted and Functional Genomics Approaches to the Mechanism of Action of Lagunamide D, a Mitochondrial Cytotoxin from Marine Cyanobacteria
Biochem Pharmacol. 2023 May 16:115608. doi: 10.1016/j.bcp.2023.115608. Online ahead of print.ABSTRACTLagunamide D, a cyanobacterial cyclodepsipeptide, exhibits potent antiproliferative activity against HCT116 colorectal cancer cells (IC50 5.1 nM), used as a model system to probe the mechanism of action. Measurements of metabolic activity, mitochondrial membrane potential, caspase 3/7 activity and cell viability indicate the rapid action of lagunamide D on mitochondrial function and downstream cytotoxic effects in HCT116 cells. Lagunamide D preferentially targets the G1 cell cycle population and arrests cells in G2/M phase ...
Source: Biochemical Pharmacology - May 18, 2023 Category: Drugs & Pharmacology Authors: Danmeng Luo Ranjala Ratnayake Kalina R Atanasova Valerie J Paul Hendrik Luesch Source Type: research

Differential regulation of histamine H < sub > 1 < /sub > receptor-mediated ERK phosphorylation by G < sub > q < /sub > proteins and arrestins
Biochem Pharmacol. 2023 May 16;213:115595. doi: 10.1016/j.bcp.2023.115595. Online ahead of print.ABSTRACTGq protein-coupled histamine H1 receptors play crucial roles in allergic and inflammatory reactions, in which the phosphorylation of extracellular signal-regulated kinase (ERK) appears to mediate the production of inflammatory cytokines. ERK phosphorylation is regulated by G protein- and arrestin-mediated signal transduction pathways. Here, we aimed to explore how H1 receptor-mediated processes of ERK phosphorylation might be differentially regulated by Gq proteins and arrestins. For this purpose, we evaluated the regul...
Source: Biochemical Pharmacology - May 18, 2023 Category: Drugs & Pharmacology Authors: Shotaro Michinaga Ayaka Nagata Ryosuke Ogami Yasuhiro Ogawa Shigeru Hishinuma Source Type: research

Targeted and Functional Genomics Approaches to the Mechanism of Action of Lagunamide D, a Mitochondrial Cytotoxin from Marine Cyanobacteria
Biochem Pharmacol. 2023 May 16:115608. doi: 10.1016/j.bcp.2023.115608. Online ahead of print.ABSTRACTLagunamide D, a cyanobacterial cyclodepsipeptide, exhibits potent antiproliferative activity against HCT116 colorectal cancer cells (IC50 5.1 nM), used as a model system to probe the mechanism of action. Measurements of metabolic activity, mitochondrial membrane potential, caspase 3/7 activity and cell viability indicate the rapid action of lagunamide D on mitochondrial function and downstream cytotoxic effects in HCT116 cells. Lagunamide D preferentially targets the G1 cell cycle population and arrests cells in G2/M phase ...
Source: Biochemical Pharmacology - May 18, 2023 Category: Drugs & Pharmacology Authors: Danmeng Luo Ranjala Ratnayake Kalina R Atanasova Valerie J Paul Hendrik Luesch Source Type: research