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Dual check point inhibitor

Ken-ichi Kusakabe, Nobuyuki Ide, Yataro Daigo, Takeshi Itoh, Takahiko Yamamoto, Eiichi Kojima, Yasunori Mitsuoka, Genta Tadano, Sachie Tagashira, Kenichi Higashino, Yousuke Okano, Yuji Sato, Makiko Inoue, Motofumi Iguchi, Takayuki Kanazawa, Yukichi Ishioka, Keiji Dohi, Yasuto Kido, Shingo Sakamoto, Shigeru Ando, Masahiro Maeda, Masayo Higaki, Hidenori Yoshizawa, Hitoshi Murai, Yusuke Nakamura
Mps1, also known as TTK, is a dual-specificity kinase that regulates the spindle assembly check point. Increased expression levels of Mps1 are observed in cancer cells, and the expression levels correlate well with tumor grade. Such evidence points to selective inhibition of Mps1 as an attractive strategy for cancer therapeutics. Starting from an aminopyridine-based lead 3a that binds to a flipped-peptide conformation at the hinge region in Mps1, elaboration of the aminopyridine scaffold at the 2- and 6-positions led to the discovery of 19c that exhibited no significant inhibition for 287 kinases as well as improved cellular Mps1 and antiproliferative activities in A549 lung carcinoma cells (cellular Mps1 IC₅₀=5...
May 1, 2015: Bioorganic & Medicinal Chemistry
L Chang, P H Graham, J Hao, J Ni, J Bucci, P J Cozzi, J H Kearsley, Y Li
The PI3K/Akt/mTOR pathway has a central role in cancer metastasis and radiotherapy. To develop effective therapeutics to improve radiosensitivity, understanding the possible pathways of radioresistance involved and the effects of a combination of the PI3K/Akt/mTOR inhibitors with radiotherapy on prostate cancer (CaP) radioresistant cells is needed. We found that compared with parent CaP cells, CaP-radioresistant cells demonstrated G0/G1 and S phase arrest, activation of cell cycle check point, autophagy and DNA repair pathway proteins, and inactivation of apoptotic proteins...
2014: Cell Death & Disease
Li Yunlan, Zheng Juan, Li Qingshan
Di-n-butyl-(2,6-difluorobenzohydroxamato)Tin(IV) (DBDFT), a potential antitumor agent against malignancies, exhibited high activities both in vitro and in vivo. Flow cytometric analysis showed that treatment with DBDFT against Human Gastric Carcinoma (SGC-7901) cells induced a concentration and time-dependent cell accumulation in the G2/M phase of the cell cycle with a parallel depletion of the percentage of cells in G0/G1, the cell apoptosis was observed by characteristic morphological changes and AnnexinV/PI dual-immunofluorescence staining...
2014: PloS One
Gugan Kothandan, Changdev G Gadhe, Seung Joo Cho
Chemokine receptors are G protein-coupled receptors that contain seven transmembrane domains. In particular, CCR2 and CCR5 and their ligands have been implicated in the pathophysiology of a number of diseases, including rheumatoid arthritis and multiple sclerosis. Based on their roles in disease, they have been attractive targets for the pharmaceutical industry, and furthermore, targeting both CCR2 and CCR5 can be a useful strategy. Owing to the importance of these receptors, information regarding the binding site is of prime importance...
2012: PloS One
Milan Surjit, Sunil K Lal
p27Kip1 is a critical regulator of the eukaryotic cell cycle. It acts as a check point protein and regulates cell cycle progression at the G1 and G1/S phase as well as predominantly blocks cell cycle progression in the absence of growth factors. Intracellular turnover of p27 is tightly regulated at the level of translation as well as by posttranslational modification. The mechanism by which p27 protein is rapidly degraded during the G1 and G1/S phase transition is well characterized. However, the process by which p27 remains extremely stable in the absence of growth factors remains unknown...
March 1, 2007: Cell Cycle
A A Memon, Sandahl B Sorensen, E Nexo
Expression of the epidermal growth factor (EGF) receptors HER1 and HER2 has been implicated in tumour growth and poor survival, whereas expression of HER3 and HER4 has been associated with improved survival of bladder cancer patients. The balance between the expression of the EGF family members may therefore have a role to play in determining the final outcome in cancer cells. To check this, we examined the effect of HER1 activation and inhibition on the expression of the EGF receptors HER3 and HER4 and ligands - the heregulins (HRGs)...
2006: Scandinavian Journal of Clinical and Laboratory Investigation
A Gabryelewicz, W Laszewicz, J Dzieniszewski, J Ciok, K Marlicz, D Bielecki, T Popiela, J Legutko, Z Knapik, E Poniewierka
Treatment with the proton pump inhibitor (omeprazole) and single antibiotic (amoxycillin), two synergistic compounds, can cure Helicobacter pylori (H. pylori) infection, but this therapy is not as effective as had been expected. However, some studies show promising results. The aim of our study was to evaluate the effect of two weeks dual-therapy with omeprazole (O) and amoxycillin (A) on gastric (GU) and duodenal ulcer (DU) patients: ulcer healing, eradication of the H. pylori and recurrence rate of the ulcer...
September 1997: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
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