Zhang, Guolin Zhang, Chi Sun, Jia'ao Xiong, Yongjian Wang, Liang Chen, Dapeng
Published in
The Journal of pharmacology and experimental therapeutics
Recent studies suggest an important role for RNA, especially non-coding RNA, in inflammatory bowel disease (IBD) and colon cancer. Drug development based on regulating RNA rather than protein is a promising new area. Phytochemicals are naturally occurring plant-derived compounds with chemical diversity, biological activity, easy availability, and l...
Lv, Chunxiao Yuan, Dongfen Cao, Yanguang
Published in
The Journal of pharmacology and experimental therapeutics
Immune checkpoint inhibitors have emerged as a frontline treatment of a variety of malignancies. However, only a subset of patients respond to these therapies, and many initial responders eventually develop resistance, leading to tumor relapse. Programmed death protein 1 is one of the checkpoint inhibitors that is expressed on activated T cells and...
Martinez, Ramon 3rd Huang, Weiliang Samadani, Ramin Mackowiak, Bryan Centola, Garrick Chen, Lijia Conlon, Ivie L Hom, Kellie Kane, Maureen A Fletcher, Steven
...
Published in
The Journal of pharmacology and experimental therapeutics
Constitutively active extracellular signal-regulated kinase (ERK1/2) signaling promotes cancer cell proliferation and survival. We previously described a class of compounds containing a 1,1-dioxido-2,5-dihydrothiophen-3-yl 4-benzenesulfonate scaffold that targeted ERK2 substrate docking sites and selectively inhibited ERK1/2-dependent functions, in...
Luzina, Irina G Lillehoj, Erik P Lockatell, Virginia K Hyun, Sang W Lugkey, Katerina N Imamura, Akihiro Ishida, Hideharu Cairo, Christopher W Atamas, Sergei P Goldblum, Simeon E
...
Published in
The Journal of pharmacology and experimental therapeutics
Pulmonary fibrosis remains a serious biomedical problem with no cure and an urgent need for better therapies. Neuraminidases (NEUs), including NEU1, have been recently implicated in the mechanism of pulmonary fibrosis by us and others. We now have tested the ability of a broad-spectrum neuraminidase inhibitor, DANA, to modulate the in vivo response...
Fischer, Holger Senn, Claudia Ullah, Mohammed Cantrill, Carina Schuler, Franz Yu, Li
Published in
The Journal of pharmacology and experimental therapeutics
P-glycoprotein (P-gp) is a major blood-brain barrier (BBB) efflux transporter. In vitro approaches, including bi-directional efflux ratio (ER), are used to measure P-gp-mediated transport, but findings can be inconsistent across models. We propose a novel, more physiologically relevant, in vitro model: uni-directional apical efflux ratio (AP-ER) - ...
Yoshii, Yukinori Wake, Hidenori Nishimura, Yoshito Teshigawara, Kiyoshi Wang, Dengli Nishibori, Masahiro
Published in
The Journal of pharmacology and experimental therapeutics
Histidine-rich glycoprotein (HRG) treatment ameliorated the survival rate of septic mice by suppressing excess immunothrombus formation. Although such findings suggested that HRG may be one of the most useful drugs for sepsis, obtaining a stable experimental system to standardize the HRG drug product is difficult to achieve using neutrophils isolat...
Komiya, Takaki Goda, Masashi Shioya, Hiroki Katsumata, Seishi
Published in
The Journal of pharmacology and experimental therapeutics
ONO-4641 is a second-generation sphingosine 1-phosphate (S1P) receptor modulator that exhibits selectivity for S1P receptors 1 and 5. Treatment with ONO-4641 leads to a reduction in magnetic resonance imaging disease measures in patients with relapsing-remitting multiple sclerosis. The objective of this study was to explore the potential impact of ...
Ronaldson, Patrick T Brzica, Hrvoje Abdullahi, Wazir Reilly, Bianca G Davis, Thomas P
Published in
The Journal of pharmacology and experimental therapeutics
Our in vivo rodent studies have shown that Organic Anion Transporting Polypeptide 1a4 (Oatp1a4) is critical for blood-to-brain transport of statins, drugs that are effective neuroprotectants. Additionally, Transforming Growth Factor-β (TGF-β) signaling via the activin receptor-like kinase 1 (ALK1) receptor regulates Oatp1a4 functional expression. T...
Minotti, Giorgio Menna, Pierantonio Camilli, Massimiliano Salvatorelli, Emanuela Reggiardo, Giorgio
Published in
The Journal of pharmacology and experimental therapeutics
Diastolic dysfunction (DD) is an early manifestation of cancer drugs cardiotoxicity. Anthracyclines are considered as more cardiotoxic than other chemotherapeutics but previous studies have shown that both anthracycline-based and nonanthracycline chemotherapy can cause an early DD, detected one week after the end of chemotherapy. Here we characteri...
Nachnani, Rahul Raup-Konsavage, Wesley M Vrana, Kent E
Published in
The Journal of pharmacology and experimental therapeutics
Medical cannabis and individual cannabinoids, such as tetrahydrocannabinol (THC) and cannabidiol (CBD), are receiving growing attention in both the media and the scientific literature. The Cannabis plant, however, produces over 100 different cannabinoids, and cannabigerol (CBG) serves as the precursor molecule for the most abundant phytocannabinoid...
