Jin, Qing-Hao Chen, Wen-Bo Xia, Ya-Nan Liu, Bing-Yu Guan, Li-Ping
A series of 2,3-dioxoindolin-N-phenylacetamide derivatives was evaluated for inhibitory activity against CDC25B and PTP1B enzymes. Most of the derivatives showed inhibitory activity against CDC25B (IC50 = 3.2-23.2 µg/mL) and PTP1B (IC50 = 2.9-21.4 µg/mL). Compound 2h showed the most inhibitory activity in vitro with IC50 values of 3.2 and 2.9 µg/mL...
Backus, Keriann M Cao, Jian Maddox, Sean M
Published in
Bioorganic & medicinal chemistry
Compounds that react irreversibly with cysteines have reemerged as potent and selective tools for altering protein function, serving as chemical probes and even clinically approved drugs. The exquisite sensitivity of human immune cell signaling pathways to oxidative stress indicates the likely, yet still underexploited, general utility of covalent ...
Vazhappilly, Cijo George Saleh, Ekram Ramadan, Wafaa Menon, Varsha Al-Azawi, Aya Mudhafar Tarazi, Hamadeh Abdu-Allah, Hajjaj El-Shorbagi, Abdel-Nasser El-Awady, Raafat
Published in
Investigational New Drugs
Kinases and phosphatases are important players in growth signaling and are involved in cancer development. For development of targeted cancer therapy, attention is given to kinases rather than phosphatases inhibitors. Src homology region 2 domain-containing protein tyrosine phosphatase2 (SHP2) is overexpressed in different types of cancers. We inve...
Heck, Karina Alvarenga, Danillo O. Shishido, Tania K. Varani, Alessandro M. Dörr, Felipe A. Pinto, Ernani Rouhiainen, Leo Jokela, Jouni Sivonen, Kaarina Fiore, Marli F.
...
Microcystins (MCs) are serine/threonine phosphatase inhibitors synthesized by several members of the phylum Cyanobacteria. Mining the draft genome sequence of the nostocalean MC-producing Fischerella sp. strain CENA161 led to the identification of three contigs containing mcy genes. Subsequent PCR and Sanger sequencing allowed the assembling of its...
Takai, Akira Eto, Masumi Hirano, Katsuya Takeya, Kosuke Wakimoto, Toshiyuki Watanabe, Masaru
Published in
The Journal of Physiological Sciences
Protein phosphatases 1 and 2A (PP1 and PP2A) are the most ubiquitous and abundant serine/threonine phosphatases in eukaryotic cells. They play fundamental roles in the regulation of various cellular functions. This review focuses on recent advances in the functional studies of these enzymes in the field of smooth muscle physiology. Many naturally o...
Fonseca, Emanuella M B Trivella, Daniela B B Scorsato, Valéria Dias, Mariana P Bazzo, Natália L Mandapati, Kishore R de Oliveira, Fábio L Ferreira-Halder, Carmen V Pilli, Ronaldo A Miranda, Paulo C M L
...
Published in
Bioorganic & medicinal chemistry
Low molecular weight protein tyrosine phosphatases (LMW-PTP, EC 3.1.3.48) are a family of single-domain enzymes with molecular weight up to 18 kDa, expressed in different tissues and considered attractive pharmacological targets for cancer chemotherapy. Despite this, few LMW-PTP inhibitors have been described to date, and the structural information...
Zhao, Shui-Lian Peng, Zhou Zhen, Xing-Hua Jin, Hong-Guo Han, Yan Qu, You-Le Guan, Li-Ping
Published in
Medicinal Chemistry Research
In this study, we examined a series of 2′,4′,6′-trihydroxychalcone derivatives for their inhibitory activity as inhibitors of CDC25B and PTP1B. The pharmacological results showed that all of the tested compounds significantly inhibited CDC25B and PTP1B phosphatase in vitro. Among them, three compounds 2, 6, and 7 had the best inhibition activity, w...
Zhang, Jian Ji, Fu-Jian Gu, Ye Zhang, Xin-Yao Qiao, Shi-Xing
Published in
Pharmacological Reports
To discover novel cell division cycle 25 (CDC25) B inhibitors and elucidate the mechanisms of inhibition in cancer cells. Nineteen 2′-hydroxy-4′-isoprenyloxychalcone derivatives (a-s) were evaluated the inhibition CDC25B activity. The enzymatic activities of the CDC25B catalytic domain were determined by monitoring the dephosphorylation of OMFP. Ce...
O’Donnell, Robert T. Pearson, David McKnight, Hayes C. Ma, Ya Peng Tuscano, Joseph M.
Published in
Cancer Immunology, Immunotherapy
PurposeTo examine the role of phosphatase inhibition on anti-CD22, HB22.7-mediated lymphomacidal effects.Experimental designCD22 is a cell-surface molecule expressed on most B cell lymphomas (NHL). HB22.7 is an anti-CD22 monoclonal antibody that binds a unique CD22-epitope, blocks ligand binding, initiates signaling, and has demonstrated lymphomaci...
Popov, Doina
Published in
Biochemical and Biophysical Research Communications
Protein Tyrosine Phosphatases (PTPs) are important contributors to vascular cells normal function, by balancing signaling proteins activation exerted by phosphorylating kinases. Type 2 diabetes related insults, such as hyperglycemia, oxidative stress, and insulin resistance disturb the phosphorylation/dephosphorylation equilibrium towards an abnorm...