Ho, Yu Siong Torres-Vergara, Pablo Penny, Jeffrey
Published in
British journal of pharmacology
Blood-brain barrier (BBB) ABCB1, ABCG2 and ABCC5 transporters influence central therapeutic drug distribution. Transporter expression is regulated by the NR3C1, NR1I3 and NR1I2 nuclear receptors, but their precise roles in brain are poorly understood. We investigated the effects of selective ligand-based activation of NR3C1, NR1I3, NR1I2 and NR2B1 ...
Xiao, Xue Chen, Sufang Huang, Ziyan Han, Xue Dou, Chaoxun Kang, Jiayi Wang, Tienan Xie, Hanbin Zhang, Linan Hei, Ziqing
...
Published in
British journal of pharmacology
Acute lung injury (ALI) is a serious, life-threatening inflammation of the lungs that still lacks effective treatment. We previously showed that serine protease inhibitor B1 (SerpinB1) protects against ALI induced by orthotopic autologous liver transplantation. However, the role of SerpinB1 in lipopolysaccharide (LPS)-induced ALI and its regulatory...
Lin, JinHeng Scullion, Lauren Garland, Christopher J Dora, Kim
Published in
British journal of pharmacology
Raised serum concentrations of the sympathetic co-transmitter neuropeptide Y (NPY) are linked to cardiovascular diseases. However, the signalling mechanism for vascular smooth muscle (VSM) constriction to NPY is poorly understood. Therefore, the present study investigated the mechanisms of NPY-induced vasoconstriction in rat small mesenteric (RMA) ...
Pökl, Michael Sridhar, Akshay Frampton, Damon J A Linhart, Veronika A Delemotte, Lucie Liin, Sara I
Published in
British journal of pharmacology
Cannabidiol (CBD) is used clinically as an anticonvulsant. Its precise mechanism of action has remained unclear. CBD was recently demonstrated to enhance the activity of the neuronal KV 7.2/7.3 channel, which may be one important contributor to CBD anticonvulsant effect. Curiously, CBD inhibits the closely related cardiac KV 7.1/KCNE1 channel. Whet...
Rajendran, Ranjithkumar Rajendran, Vinothkumar Böttiger, Gregor Stadelmann, Christine Shirvanchi, Kian von Au, Laureen Bhushan, Sudhanshu Wallendszus, Natascha Schunin, Darja Westbrock, Victor
...
Published in
British journal of pharmacology
Fibroblast growth factors and receptors (FGFR) have been shown to modulate inflammation and neurodegeneration in multiple sclerosis (MS). The selective FGFR inhibitor infigratinib has been shown to be effective in cancer models. Here, we investigate the effects of infigratinib on prevention and suppression of first clinical episodes of myelin oligo...
Cheng, Li-Zhi Huang, Dan-Ling Tang, Zhang-Rui Zhang, Jia-Hao Xiong, Ting Zhou, Chen Zhang, Nai-Xia Fu, Rong Cheng, Yong-Xian Wu, Zhao-Qiu
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Published in
British journal of pharmacology
The scaffold molecule Axin2 is constitutively activated in colorectal cancer (CRC) and functions as a potent promoter of CRC behaviour. Pharmacological targeting of Axin2 may therefore exert a therapeutic effect in patients with CRC. Here, we discovered a potent small-molecule inhibitor of Axin2, based on the mechanism by which Axin2 is regulated p...
Kim, Chaeeun Kim, Yerin Lim, Ji Yeon Kim, Minseok Zheng, Haiyan Kim, Miri Hwang, Sun Wook
Published in
British journal of pharmacology
Pruritic dermatitis is a disease with a considerable unmet need for treatment and appears to present with not only epidermal but also peripheral neuronal complications. Here, we propose a novel pharmacological modulation targeting both peripheral dorsal root ganglion (DRG) sensory neurons and skin keratinocytes. GPR35 is an orphan G-protein-coupled...
Xu, Qingping Cao, Yuhong Zhong, Xiaoyi Qin, Xue Feng, Jingyun Peng, Huan Su, Yongshao Ma, Zhichao Zhou, Sigui
Published in
British journal of pharmacology
Our recent studies have shown that flavin adenine dinucleotide (FAD) exerts cardiovascular protective effects by supplementing short-chain acyl-CoA dehydrogenase (SCAD). The current study aimed to elucidate whether riboflavin (the precursor of FAD) could improve heart failure via activating SCAD and the DJ-1-Keap1-Nrf2 signalling pathway. Riboflavi...
Kaur, Harmandeep Yerra, Veera Ganesh Batchu, Sri Nagarjun Tran, Duc Tin Kabir, M D Golam Liu, Youan Advani, Suzanne L Sedrak, Phelopater Geldenhuys, Laurette Tennankore, Karthik K
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Published in
British journal of pharmacology
Activated fibroblasts deposit fibrotic matrix in chronic kidney disease (CKD) and G-protein coupled receptors (GPCRs) are the most druggable therapeutic targets. Here, we set out to establish a transcriptional profile that identifies activated kidney fibroblasts and the GPCRs that they express. RNA sequencing and single cell qRT-PCR were performed ...
Ranasinghe, Priyanga Addison, Melisande L Dear, James W Webb, David J
Published in
British journal of pharmacology
Post-transcriptional gene silencing targets and degrades mRNA transcripts, silencing the expression of specific genes. RNA interference technology, using synthetic structurally well-defined short double-stranded RNA (small interfering RNA [siRNA]), has advanced rapidly in recent years. This introductory review describes the utility of siRNA, by exp...
