Parcourir par sujet "drug screening"

4-Arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects

Kryštof, V.; Cankař, P.; Fryšová, I.; Slouka, J.; Kontopidis, G.; Džubák, P.; Hajdúch, M.; Srovnal, J.; De Azevedo Jr, W. F.; Orság, M.; Paprskářová, M.; Rolčík, J.; Látr, A.; Fischer, P. M.; Strnad, M. (2006)

In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR ...

Advanced Non-linear Mathematical Model for the Prediction of the Activity of a Putative Anticancer Agent in Human-to-mouse Cancer Xenografts

Liliopoulos S.G., Stavrakakis G.S., Dimas K.S. (2020)

Background/Aim: Mathematical models have long been considered as important tools in cancer biology and therapy. Herein, we present an advanced non-linear mathematical model that can predict accurately the effect of an ...

Annonacin promotes selective cancer cell death via NKA-dependent and SERCA-dependent pathways

Yiallouris A., Patrikios I., Johnson E.O., Sereti E., Dimas K., De Ford C., Fedosova N.U., Graier W.F., Sokratous K., Kyriakou K., Stephanou A. (2018)

In the healthcare sector, phytocompounds are known to be beneficial by contributing or alleviating a variety of diseases. Studies have demonstrated the progressive effects of phytocompounds on immune-related diseases and ...

Anti-invasive effects of CXCR4 and FAK inhibitors in non-small cell lung carcinomas with mutually inactivated p53 and PTEN tumor suppressors

Dragoj M., Bankovic J., Sereti E., Stojanov S.J., Dimas K., Pesic M., Stankovic T. (2017)

Non-small cell lung carcinoma (NSCLC) is the most common type of lung cancer. At the time of diagnosis, a large percentage of NSCLC patients have already developed metastasis, responsible for extremely high mortality rates. ...

Anticancer and apoptosis-inducing effects of quercetin in vitro and in vivo

Hashemzaei M., Far A.D., Yari A., Heravi R.E., Tabrizian K., Taghdisi S.M., Sadegh S.E., Tsarouhas K., Kouretas D., Tzanakakis G., Nikitovic D., Anisimov N.Y., Spandidos D.A., Tsatsakis A.M., Rezaee R. (2017)

The present study focused on the elucidation of the putative anticancer potential of quercetin. The anticancer activity of quercetin at 10, 20, 40, 80 and 120 μM was assessed in vitro by MMT assay in 9 tumor cell lines ...

Antiviral unsaturates nucleosides

Komiotis, D.; Manta, S.; Tsoukala, E.; Tzioumaki, N. (2008)

In the search for effective, selective and nontoxic antiviral agents, a variety of nucleoside analogues have been synthesized, with different functionalities in the carbohydrate moiety. Unsaturated nucleoside analogues are ...

Characterization and Quantitative Determination of a Diverse Group of Bacillus subtilis subsp. subtilis NCIB 3610 Antibacterial Peptides

Karagiota A., Tsitsopoulou H., Tasakis R.N., Zoumpourtikoudi V., Touraki M. (2021)

Five antibacterial peptides produced by Bacillus subtilis NCIB 3610 were purified, quantified, characterized, and identified in the present study. Cell-free extracts were subjected to three purification protocols employing ...

Chios mastic gum: A plant-produced resin exhibiting numerous diverse pharmaceutical and biomedical prοperties

Dimas, K. S.; Pantazis, P.; Ramanujam, R. (2012)

Chios mastic gum (CMG) is a resin produced by the plant Pistacia lentiscus var. chia. CMG is used to extract the mastic gum essential oil (MGO). CMG and MGO consist of nearly 70 constituents and have demonstrated numerous ...

Current status and future prospects of small–molecule protein–protein interaction (PPI) inhibitors of tumor necrosis factor (TNF) and receptor activator of NF-κB ligand (RANKL)

Melagraki G., Leonis G., Ntougkos E., Rinotas V., Papaneophytou C., Mavromoustakos T., Kontopidis G., Douni E., Kollias G., Afantitis A. (2018)

The overexpression of Tumor Necrosis Factor (TNF) is directly related to the development of several autoimmune diseases, such as rheumatoid and psoriatic arthritis, inflammatory bowel disease, Crohn’s disease, refractory ...

Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors

McIntyre, N. A.; McInnes, C.; Griffiths, G.; Barnett, A. L.; Kontopidis, G.; Slawin, A. M. Z.; Jackson, W.; Thomas, M.; Zheleva, D. I.; Wang, S.; Blake, D. G.; Westwood, N. J.; Fischer, P. M. (2010)

Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- ...

Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents

Wang, S.; Griffiths, G.; Midgley, C. A.; Barnett, A. L.; Cooper, M.; Grabarek, J.; Ingram, L.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; McLachlan, J.; Meades, C.; Mezna, M.; Stuart, I.; Thomas, M. P.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Blake, D. G.; Fischer, P. M. (2010)

The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity, since the ATP-binding motif is present in many proteins. We introduce a strategy that has allowed us to identify compounds ...

Discovery of Small-Molecule Inhibitors of Receptor Activator of Nuclear Factor-κB Ligand with a Superior Therapeutic Index

Rinotas V., Papakyriakou A., Violitzi F., Papaneophytou C., Ouzouni M.-D., Alexiou P., Strongilos A., Couladouros E., Kontopidis G., Eliopoulos E., Douni E. (2020)

Receptor activator of nuclear factor-κB ligand (RANKL) constitutes the master mediator of osteoclastogenesis, while its pharmaceutical inhibition by a monoclonal antibody has been approved for the treatment of postmenopausal ...

An evaluation of indirubin analogues as phosphorylase kinase inhibitors

Begum, J.; Skamnaki, V. T.; Moffatt, C.; Bischler, N.; Sarrou, J.; Skaltsounis, A. L.; Leonidas, D. D.; Oikonomakos, N. G.; Hayes, J. M. (2015)

Phosphorylase kinase (PhK) has been linked with a number of conditions such as glycogen storage diseases, psoriasis, type 2 diabetes and more recently, cancer (Camus et al., 2012 [6]). However, with few reported structural ...

Functional characterization and anti-cancer action of the clinical phase II cardiac Na+/K+ ATPase inhibitor istaroxime: In vitro and in vivo properties and cross talk with the membrane androgen receptor

Alevizopoulos K., Dimas K., Papadopoulou N., Schmidt E.-M., Tsapara A., Alkahtani S., Honisch S., Prousis K.C., Alarifi S., Calogeropoulou T., Lang F., Stournaras C. (2016)

Sodium potassium pump (Na+/K+ ATPase) is a validated pharmacological target for the treatment of various cardiac conditions. Recent published data with Na+/K+ ATPase inhibitors suggest a potent anti-cancer action of these ...

Glycogen phosphorylase as a target for type 2 diabetes: Synthetic, biochemical, structural and computational evaluation of novel N-acyl-N´-(β-D-glucopyranosyl) urea inhibitors

Kantsadi, A. L.; Parmenopoulou, V.; Bakalov, D. N.; Snelgrove, L.; Stravodimos, G. A.; Chatzileontiadou, D. S. M.; Manta, S.; Panagiotopoulou, A.; Hayes, J. M.; Komiotis, D.; Leonidas, D. D. (2015)

Glycogen phosphorylase (GP), a validated target for the development of anti-hyperglycaemic agents, has been targeted for the design of novel glycopyranosylamine inhibitors. Exploiting the two most potent inhibitors from ...

Local intracerebral inhibition of IRE1 by MKC8866 sensitizes glioblastoma to irradiation/chemotherapy in vivo

Le Reste P.J., Pineau R., Voutetakis K., Samal J., Jégou G., Lhomond S., Gorman A.M., Samali A., Patterson J.B., Zeng Q., Pandit A., Aubry M., Soriano N., Etcheverry A., Chatziioannou A., Mosser J., Avril T., Chevet E. (2020)

Glioblastoma multiforme (GBM) is the most severe primary brain cancer. Despite an aggressive treatment comprising surgical resection and radio/chemotherapy, patient's survival post diagnosis remains short. A limitation for ...

Meta-analysis Evaluating the Effect of Sodium-Glucose Co-Transporter-2 Inhibitors on the Risk for New-Onset Obstructive Sleep Apnea in Patients With Type 2 Diabetes Mellitus Regardless of Cardiovascular Disease at Baseline

Patoulias D., Dimosiari A., Michailidis T., Roditis P., Lampropoulos S. (2022)

[No abstract available]

Multicomponent reaction of aldehydes, amines and oxalacetate analogues leading to biologically attractive pyrrole derivatives

Manta S., Kollatos N., Mitsos C., Chatzieffraimidi G.-A., Papanastasiou I., Gallos J.K., Komiotis D. (2020)

Pyrrole is a very important pharmacophoric moiety. It has been widely incorporated into the skeleton of antitumor, anti-inflammatory, antibacterial, antioxidant and antifungal active substances. Access to this key heterocycle ...

A multidisciplinary study of 3-(β-D-glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors

Kun S., Begum J., Kyriakis E., Stamati E.C.V., Barkas T.A., Szennyes E., Bokor É., Szabó K.E., Stravodimos G.A., Sipos Á., Docsa T., Gergely P., Moffatt C., Patraskaki M.S., Kokolaki M.C., Gkerdi A., Skamnaki V.T., Leonidas D.D., Somsák L., Hayes J.M. (2018)

3-(β-D-Glucopyranosyl)-5-substituted-1,2,4-triazoles have been revealed as an effective scaffold for the development of potent glycogen phosphorylase (GP) inhibitors but with the potency very sensitive to the nature of the ...

The novel dehydroepiandrosterone (DHEA) derivative BNN27 counteracts behavioural deficits induced by the NMDA receptor antagonist ketamine in rats

Zoupa E., Gravanis A., Pitsikas N. (2019)

Consistent experimental evidence supports an important role of the glutamatergic system in the etiopathogenesis of schizophrenia. Numerous studies propose that blockade of the NMDA receptor by its antagonist ketamine impairs ...