Characterization of novel Checkpoint kinase 1 inhibitors by in vitro assays and in human cancer cells treated with topoisomerase inhibitors

Life Sciences ◽  
2011 ◽  
Vol 89 (7-8) ◽  
pp. 259-268 ◽  
Author(s):  
Gilles Ferry ◽  
Aurélie Studeny ◽  
Céline Bossard ◽  
Philip M. Kubara ◽  
Denis Zeyer ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
In Vitro Assays ◽  
Topoisomerase Inhibitors ◽  
Checkpoint Kinase ◽  
Checkpoint Kinase 1 ◽  
Human Cancer Cells

Structural characterization of new zinc(ii) complexes with N2O2 chelating thiosemicarbazidato ligands; investigation of the relationship between their DNA interaction and in vitro antiproliferative activity towards human cancer cells

2020 ◽  
Vol 44 (22) ◽  
pp. 9313-9320
Author(s):  
Büşra Kaya ◽  
Zehra Kübra Yılmaz ◽  
Onur Şahin ◽  
Belma Aslim ◽  
Bahri Ülküseven
Keyword(s):  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Dna Interaction ◽  
Antiproliferative Agents ◽  
Human Cancer Cells ◽  
Dna Targeting ◽  
The Relationship

New candidates to become DNA-targeting antiproliferative agents: Zinc(ii) complexes bearing N2O2-thiosemicarbazidato ligands.

scholarly journals In Vitro Characterization of an Anti-HER2 Affibody-Monomethyl Auristatin E Conjugate in HER2-Positive Breast Cancer Cells

2021 ◽  
Vol 7 (1) ◽  
pp. 3
Author(s):  
Isabella Damiani ◽  
Silvia Castiglioni ◽  
Valentina Rusconi ◽  
Clara Rossi ◽  
Alberto Corsini ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Binding Affinities ◽  
Her2 Positive ◽  
Human Cancer Cells ◽  
Protein Levels ◽  
Drug Conjugates ◽  
In Vitro Characterization

Antibody-drug conjugates (ADCs) are used in anticancer therapy with some limitations due to their molecular properties. An alternative to monoclonal antibodies is the affibody, composed of 58 amino acids, with lower binding affinities, small size, and rapid blood clearance and tissue distribution. We investigate the in vitro efficacy of a novel anti-HER2 ZHER2:2891 affibody conjugated to a cytotoxic drug auristatin E (MMAE) in HER2-positive human cancer cells. An adenocarcinoma cell line SK-BR-3, expressing high levels of HER2, and mammary gland adenocarcinoma MDA-MB-231, expressing basal levels of HER2, were treated with ZHER2:2891DCS-MMAE and trastuzumab (as a reference compound). ZHER2:2891DCS-MMAE induced a significant time-dependent toxic effect in SK-BR-3 cells. A 30% reduction in cell viability was found after 10 min exposure at 7 nM with an IC50 of 80.2 nM. On the contrary, MDA-MB-231 cells were not affected by the affibody complex. The HER2-specific cytotoxic effect of the ZHER2:2891DCS-MMAE has also been confirmed by measuring apoptosis by flow cytometry. In SK-BR-3 cells, the increasing concentrations of the conjugated affibody induced cell death after 10 min of treatment with the strongest effect observed after 48 h. Moreover, treatment with ZHER2:2891DCS-MMAE reduced (up to 50%) HER2 expression at both mRNA and protein levels in SK-BR-3 cells after 24 h of treatment. In conclusion, the cytotoxic conjugate based on the anti-HER2 affibody and MMAE efficiently interacts with HER2 over-expressing cancer cells, allowing the selective and specific delivery of the cytotoxic payload. The basal HER2 expressing cells are not the most affected probably due to a lower uptake of the drug conjugate. This confirms that affibodies may be used to target HER2 overexpressing cells while sparing normal cells.

scholarly journals A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo

2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Antitumour Activity ◽  
Anticancer Compounds ◽  
Human Cancer Cells ◽  
Cycle Arrest ◽  
Apoptosis Inducer ◽  
Purine Ring

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer.

Rhodium(i) N-heterocyclic carbene complexes: synthesis and cytotoxic properties

2021 ◽  
Vol 45 (11) ◽  
pp. 5176-5183
Author(s):  
Ichraf Slimani ◽  
Serap Şahin-Bölükbaşı ◽  
Mustafa Ulu ◽  
Enes Evren ◽  
Nevin Gürbüz ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Mtt Assay ◽  
Incubation Time ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Carbene Complexes ◽  
Human Cancer Cells ◽  
Benzimidazolium Salts ◽  
Ht 29

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.

Multicomponent 5-fluorouracil loaded PAMAM stabilized-silver nanocomposites synergistically induce apoptosis in human cancer cells

2015 ◽  
Vol 3 (3) ◽  
pp. 457-468 ◽  
Author(s):  
Ishita Matai ◽  
Abhay Sachdev ◽  
P. Gopinath
Keyword(s):  
Cancer Therapy ◽  
Cancer Cells ◽  
Therapeutic Agent ◽  
Human Cancer ◽  
Pamam Dendrimer ◽  
Human Cancer Cells ◽  
Silver Nanocomposites

Herein, we report the development of a poly(amidoamine) (PAMAM) dendrimer based multicomponent therapeutic agent forin vitrocancer therapy applications.

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