Yan, Zhao Huina, Wu Xiaoyan, Xing Yuqian, Ma Shengping, Ji Xinyue, Xu Xin, Zhao Sensen, Wang Wenyan, Jiang Chunyan, Fang
...
Published in
The Journal of pharmacology and experimental therapeutics
Chemoresistance of hepatocellular carcinoma is one of the most serious problems, which directly hinders the effect of chemotherapy agents. We previously reported that CD13 inhibition can enhance the cytotoxic efficacy of chemotherapy agents. In the present study, we utilizes liver cancer cell to explore molecular mechanism accounting for the relati...
Fischer, Deborah P Griffiths, Anna L Lui, Sylvia Sabar, Uzmah J Farrar, Diane O'Donovan, Peter J Woodward, David F Marshall, Kay M
Published in
The Journal of pharmacology and experimental therapeutics
Prostaglandin (PG) E analogues are used clinically to ripen the cervix and induce labour. However, selective receptor agonists may have potential to improve induction response rates or manage unwanted uterine hypercontractility in conditions such as dysmenorrhoea and preterm labour. To characterise their therapeutic value, PGE2 analogues were used ...
Cui, Wenqi Shen, Xunan Agbas, Emre Tompkins, Brandon Cameron-Carter, Hadley Staudinger, Jeff
Published in
The Journal of pharmacology and experimental therapeutics
The pregnane x receptor (PXR, NR1I2) is a ligand-activated nuclear receptor (NR) superfamily member that is enriched in liver and intestine in mammals. Activation of PXR regulates the expression of genes encoding key proteins involved in drug metabolism, drug efflux and drug transport. Recent mechanistic investigations reveal that post-translationa...
Xu, Li-Hua Yang, Yao Liu, Hong-Xia Xiao, Shui-Feng Qiu, Wen-Xia Wang, Jin-Xing Zhao, Chen-Chen Gui, Yuan-Hong Liu, Gui-Zhu Peng, Bin
...
Published in
The Journal of pharmacology and experimental therapeutics
It has been identified that arginine vasopressin (AVP), AVP receptor 2 (V2R) and the aquaporin 2 (AQP2) signaling pathway in the inner ear play important roles in hearing and balance functions through regulating the endolymph equilibrium; however, the contributions of this signaling pathway to the development of motion sickness are unclear. The pre...
Singh, Ashvani K Fan, Yihong Balut, Corina Alani, Sara Manelli, Arlene M Swensen, Andrew M Jia, Ying Neelands, Torben R Vortherms, Timothy A Liu, Bo
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Published in
The Journal of pharmacology and experimental therapeutics
Cystic fibrosis (CF) is the most common monogenic autosomal recessive disease in Caucasians caused by pathogenic mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene (CFTR). Significant small molecule therapeutic advances over the past two decades have been made to target the defective CFTR protein and enhance its functi...
Chen, Yen-Chu Fowler, James P Wang, Jing Watson, Christy J W Sherafat, Yasmine Staben, Andres Lazarus, Philip Denton, Travis T Fowler, Christie D
Published in
The Journal of pharmacology and experimental therapeutics
During tobacco and e-cigarette use, nicotine is mainly metabolized in the human liver by cytochrome P450 2A6 (CYP2A6). Given that a slower CYP2A6 metabolism has been associated with less vulnerability to develop nicotine dependence, the current studies sought to validate a novel CYP2A6 inhibitor, (5-(4-ethylpyridin-3-yl)thiophen-2-yl)methanamine (D...
Witkin, Jeffrey M Li, Guanguan Golani, Lalit K Xiong, Wenhui Smith, Jodi L Ping, Xingjie Rashid, Farjana Jahan, Rajwana Cerne, Rok Cook, James M
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Published in
The Journal of pharmacology and experimental therapeutics
The imidizodiazepine, 5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole (KRM-II-81), is selective for α2/3-containing GABAA receptors. KRM-II-81 dampens seizure activity in rodent models with enhanced efficacy and reduced motor-impairment compared with diazepam. In the present study, KRM-II-81 was studied in assays d...
Marek, Gerard J Cunningham, Kathryn A Rasmussen, Kurt
Published in
The Journal of pharmacology and experimental therapeutics
Withey, Sarah L Spealman, Roger D Bergman, Jack Paronis, Carol A
Published in
The Journal of pharmacology and experimental therapeutics
Buprenorphine, a partial agonist at the μ-opioid receptor, is commonly prescribed for the management of opioid addiction. Notwithstanding buprenorphine's clinical popularity, the relationship between its effectiveness in attenuating relapse-related behavior and its opioid efficacy is poorly understood. Furthermore, changes in the antinociceptive po...
Farrell, Pamela J Zopf, Christopher J Huang, Huey-Jing Balakrishna, Deepika Holub, Corine Bilakovics, James Fanjul, Andrea Matuszkiewicz, Jennifer Plonowski, Artur Rolzin, Paul
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Published in
The Journal of pharmacology and experimental therapeutics
Target-engagement pharmacodynamic (PD) biomarkers are valuable tools in the prioritization of drug candidates, especially for novel, first-in-class mechanisms whose robustness to alter disease outcome is unknown. Methionine aminopeptidase 2 (MetAP2) is a cytosolic metalloenzyme that cleaves the N-terminal methionine from nascent proteins. Inhibitio...
