Telomerase inhibitors: a new option for chemotherapy

2003 ◽  
pp. 31-58 ◽  
Author(s):  
Zhi Chen ◽  
David R. Corey
Keyword(s):  
Telomerase Inhibitors

Telomerase Inhibitors: Potential Anticancer Agents

2016 ◽  
Vol 13 (1) ◽  
pp. 49-61 ◽  
Author(s):  
Rakesh R. Somani ◽  
Mayuri H. Patel
Keyword(s):  
Anticancer Agents ◽  
Telomerase Inhibitors

scholarly journals Design and study of telomerase inhibitors based on G-quadruplex ligands

2013 ◽  
Vol 29 (3) ◽  
pp. 169-176 ◽  
Author(s):  
V. V. Negrutska ◽  
L. V. Dubey ◽  
M. M. Ilchenko ◽  
I. Ya. Dubey
Keyword(s):  
Telomerase Inhibitors ◽  
G Quadruplex

Eine konvergente Totalsynthese des Telomerase-Inhibitors (±)-γ-Rubromycin

2014 ◽  
Vol 126 (17) ◽  
pp. 4420-4424 ◽  
Author(s):  
Michael Wilsdorf ◽  
Hans-Ulrich Reißig
Keyword(s):  
Telomerase Inhibitors

Novel ruthenium(ii) polypyridyl complexes as G-quadruplex stabilisers and telomerase inhibitors

2014 ◽  
Vol 43 (21) ◽  
pp. 7811 ◽  
Author(s):  
Guoliang Liao ◽  
Xiang Chen ◽  
Jingheng Wu ◽  
Chen Qian ◽  
Hanqiang Wang ◽  
...  
Keyword(s):  
Polypyridyl Complexes ◽  
Telomerase Inhibitors ◽  
G Quadruplex

scholarly journals Selective Binding of Distamycin A Derivative to G-Quadruplex Structure [d(TGGGGT)]4

2010 ◽  
Vol 2010 ◽  
pp. 1-7 ◽  
Author(s):  
Bruno Pagano ◽  
Iolanda Fotticchia ◽  
Stefano De Tito ◽  
Carlo A. Mattia ◽  
Luciano Mayol ◽  
...  
Keyword(s):  
Small Molecules ◽  
Titration Calorimetry ◽  
Distamycin A ◽  
Structural Modifications ◽  
Telomerase Inhibitors ◽  
G Quadruplex ◽  
Nmr Techniques ◽  
Eukaryotic Organisms ◽  
New Anticancer Drugs ◽  
Binding Behaviour

Guanine-rich nucleic acid sequences can adopt G-quadruplex structures stabilized by layers of four Hoogsteen-paired guanine residues. Quadruplex-prone sequences are found in many regions of human genome and in the telomeres of all eukaryotic organisms. Since small molecules that target G-quadruplexes have been found to be effective telomerase inhibitors, the identification of new specific ligands for G-quadruplexes is emerging as a promising approach to develop new anticancer drugs. Distamycin A is known to bind to AT-rich sequences of duplex DNA, but it has recently been shown to interact also with G-quadruplexes. Here, isothermal titration calorimetry (ITC) and NMR techniques have been employed to characterize the interaction between a dicationic derivative of distamycin A (compound1) and the [d(TGGGGT)]4quadruplex. Additionally, to compare the binding behaviour of netropsin and compound1to the same target, a calometric study of the interaction between netropsin and [d(TGGGGT)]4has been performed. Experiments show that netropsin and compound1are able to bind to [d(TGGGGT)]4with good affinity and comparable thermodynamic profiles. In both cases the interactions are entropically driven processes with a small favourable enthalpic contribution. Interestingly, the structural modifications of compound1decrease the affinity of the ligand toward the duplex, enhancing the selectivity.

Telomerase inhibitors as novel antitumor drugs

2011 ◽  
Vol 47 (7) ◽  
pp. 655-660 ◽  
Author(s):  
A. I. Glukhov ◽  
L. V. Svinareva ◽  
S. E. Severin ◽  
V. I. Shvets
Keyword(s):  
Antitumor Drugs ◽  
Telomerase Inhibitors

Design Potent Telomerase Inhibitors Using Structure Based Approaches

2019 ◽  
pp. 60-63
Author(s):  
Shalini Bajaj ◽  
Nilofer Gerald Arakal ◽  
Manikanta Murahari ◽  
Mayur C. Yergeri
Keyword(s):  
Telomerase Inhibitors

scholarly journals The Role of Alternative Lengthening of Telomeres Mechanism in Cancer: Translational and Therapeutic Implications

Cancers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 949 ◽  
Author(s):  
Marta Recagni ◽  
Joanna Bidzinska ◽  
Nadia Zaffaroni ◽  
Marco Folini
Keyword(s):  
Cancer Cells ◽  
Tumor Biology ◽  
Telomerase Activity ◽  
Telomere Maintenance ◽  
Limited Information ◽  
Adaptive Responses ◽  
Therapeutic Implications ◽  
Telomerase Inhibitors ◽  
Alternative Lengthening

Telomere maintenance mechanisms (i.e., telomerase activity (TA) and the alternative lengthening of telomere (ALT) mechanism) contribute to tumorigenesis by providing unlimited proliferative capacity to cancer cells. Although the role of either telomere maintenance mechanisms seems to be equivalent in providing a limitless proliferative ability to tumor cells, the contribution of TA and ALT to the clinical outcome of patients may differ prominently. In addition, several strategies have been developed to interfere with TA in cancer, including Imetelstat that has been the first telomerase inhibitor tested in clinical trials. Conversely, the limited information available on the molecular underpinnings of ALT has hindered thus far the development of genuine ALT-targeting agents. Moreover, whether anti-telomerase therapies may be hampered or not by possible adaptive responses is still debatable. Nonetheless, it is plausible hypothesizing that treatment with telomerase inhibitors may exert selective pressure for the emergence of cancer cells that become resistant to treatment by activating the ALT mechanism. This notion, together with the evidence that both telomere maintenance mechanisms may coexist within the same tumor and may distinctly impinge on patients’ outcomes, suggests that ALT may exert an unexpected role in tumor biology that still needs to be fully elucidated.

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