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Publikováno v:
Biochemical Pharmacology. 168:214-223
Targeting Trp-Kyn pathways has been identified as an attractive approach for the cancer immunotherapies. In this study, a novel phosphonamidate containing compound was designed, synthesized and evaluated for its inhibitory activity against key dioxyg
Autor:
Wayne E. Childers, Yaroslava Karpova, Mark E. McDonnell, John Gordon, Peter Makhov, Elizabeth Hewlett, Tomasz Skorski, Alexei V. Tulin, Allen B. Reitz, Vladimir Kolenko, Chao Wu, Ali Divan, Min Ye
Publikováno v:
Biochem Pharmacol
In our previous studies of the molecular mechanisms of poly(ADP-ribose) polymerase 1 (PARP-1)-mediated transcriptional regulation we identified a novel class of PARP-1 inhibitors targeting the histone-dependent route of PARP-1 activation. Because his
Autor:
Claire Hull, Sarah Kamli-Salino, Victor A. Gault, Shakil Khan, Bettina Platt, Nicola Morrice, Nimesh Mody, Kaja Plucinska, Ruta Dekeryte, Mirela Delibegovic, Christopher McLaughlin
Publikováno v:
Biochemical Pharmacology. 166:222-230
We recently reported that brain-specific human β-secretase 1 (BACE1) knock-in (PLB4), a mouse model of sporadic Alzheimer's disease (AD), also develops a severe diabetic phenotype characterised by impaired glucose homeostasis, decreased insulin sens
Publikováno v:
Biochemical Pharmacology. 164:283-288
Liver slices from starved rats and incubated without other substrates oxidized ethanol at a rate of 4.1 µmols • h−1 • g−1. Addition of 10 mmols • L−1 lactate increased this rate 2-fold. 4-methylpyrazole (4-MP), an alcohol dehydrogenase (
Autor:
Adam Lesner, Artur Giełdoń, Francis Gauthier, Conni Lauritzen, Dieter E. Jenne, Maria Håkansson, Derek T. Logan, Brice Korkmaz, Magdalena Wysocka, John Pedersen
Publikováno v:
Biochemical Pharmacology
Biochemical Pharmacology, 2019, 164, pp.349-367. ⟨10.1016/j.bcp.2019.04.006⟩
Biochemical Pharmacology, 2019, 164, pp.349-367. ⟨10.1016/j.bcp.2019.04.006⟩
International audience; Cathepsin C (CatC) is a dipeptidyl-exopeptidase which activates neutrophil serine protease precursors (elastase, proteinase 3, cathepsin G and NSP4) by removing their N-terminal propeptide in bone marrow cells at the promyeloc
Autor:
Taizhen Liang, Chenliang Zhou, Fangyuan Lai, Lin Li, Shuwen Liu, Xing-hua Tan, Xuanxuan Zhang, Xinfeng Xu, Jian Lin
Publikováno v:
Biochemical Pharmacology. 164:237-251
The persistence of latent human immunodeficiency virus type 1 (HIV-1) reservoirs remains a major hurdle for HIV-1 eradication. The "shock and kill" strategy relies on the drug-mediated reversion of HIV-1 latency and the subsequent death of HIV-produc
Publikováno v:
Biochemical Pharmacology. 164:252-262
Renin-angiotensin-aldosterone system (RAS) has been implicated in non-alcoholic fatty liver disease (NAFLD); the most common cause of chronic liver diseases. There is accumulating evidence that altered TLR4 and Sphingosine kinase 1(SphK1)/sphingosine
Autor:
Francesco Violi, Daniele Pastori, Lucia Stefanini, Simona Bartimoccia, Cristina Nocella, Romano Silvestri, Vittoria Cammisotto, Roberto Carnevale, Antonio Coluccia, Pasquale Pignatelli
Publikováno v:
Biochemical Pharmacology. 163:111-118
Factor Xa (FXa) has been reported to activate platelet via interaction with glycoprotein (GP) VI but the underlying mechanism has not been fully elucidated. We investigated if Nox2-derived oxidative stress is implicated in FXa-induced platelet aggreg
Autor:
Duan fang Liao, Man Sau Wong, Nan Chen, Zhe Shi, Ming chao He, Yongjun Wang, Nan nan Sha, Ti fei Yuan, Yan Zhang, Xiao-Li Dong, Shi yu Peng
Publikováno v:
Biochemical Pharmacology. 163:1-8
Depression is highly prevalent in patients suffering from chronic inflammatory diseases. Dysregulated neuroinflammation and concomitant activated microglia play a pivotal role in the pathogenesis of depression. Paricalcitol (Pari), a vitamin D2 analo
Autor:
Wonhwa Lee, Changhun Lee, Gyu-Yong Song, Jong-Sup Bae, Yuseok O, Jee Hyun Lee, So Yeon Jeong, Moon-Chang Baek
Publikováno v:
Biochemical Pharmacology. 163:260-268
In the present study, several decursin analogues (KC1-3) were synthesized and evaluated in terms of their anti-septic activities on high mobility group box 1 (HMGB1)-mediated septic responses and survival rate in a mouse model of sepsis. KC1 and KC3,