scholarly journals Potent and selective in vitro and in vivo antiproliferative effects of metal–organic trefoil knots

2019 ◽  
Vol 10 (23) ◽  
pp. 5884-5892 ◽  
Author(s):  
Farah Benyettou ◽  
Thirumurugan Prakasam ◽  
Anjana Ramdas Nair ◽  
Ini-Isabee Witzel ◽  
Marwa Alhashimi ◽  
...  

A set of metal–organic trefoil knots (M-TKs) generated by metal-templated self-assembly of a simple pair of chelating ligands were well tolerated in vitro by non-cancer cells but were significantly more potent than cisplatin in both human cancer cells––including those resistant to cisplatin––and in zebrafish embryos.

2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  

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.


2019 ◽  
Vol 71 (1) ◽  
pp. 165-180 ◽  
Author(s):  
Tomasz Kowalczyk ◽  
Przemysław Sitarek ◽  
Ewa Skała ◽  
Monika Toma ◽  
Marzena Wielanek ◽  
...  

2009 ◽  
Vol 8 (1) ◽  
pp. 11 ◽  
Author(s):  
Keqiang Zhang ◽  
Shuya Hu ◽  
Jun Wu ◽  
Linling Chen ◽  
Jianming Lu ◽  
...  

2014 ◽  
Vol 110 ◽  
pp. S104
Author(s):  
D. Viertl ◽  
A. Annibaldi ◽  
O. Matzinger ◽  
M.-C. Vozenin ◽  
C. Widmann ◽  
...  

2018 ◽  
Vol 9 ◽  
Author(s):  
Yi-Wen Wu ◽  
Kai-Cheng Hsu ◽  
Hsueh-Yun Lee ◽  
Tsui-Chin Huang ◽  
Tony E. Lin ◽  
...  

2008 ◽  
Vol 4 (4) ◽  
pp. 318-329 ◽  
Author(s):  
Chengli Yang ◽  
Antonina Rait ◽  
Kathleen F. Pirollo ◽  
John A. Dagata ◽  
Natalia Farkas ◽  
...  

2010 ◽  
Vol 78 (3) ◽  
pp. S655-S656
Author(s):  
A.M. Vaccaro ◽  
I.K. Kandela ◽  
A.N. Pinchuk ◽  
N.J. Fleck ◽  
J.P. Weichert ◽  
...  

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