Telomerase inhibitors: a patent review (2010-2015).
BACKGROUND
Telomerase is a ribonucleoprotein that catalyses the addition of telomeric repeat sequences (having the sequence 5'-TTAGGG-3' in humans) to the ends of chromosomes. Telomerase activity is detected in most types of human tumours, but it is almost undetectable in normal somatic cells. Therefore, telomerase is a promising therapeutic target. To date, the known inhibitors of telomerase include nucleoside analogues, oligonucleotides and G-quadruplex stabilizers. This review highlights recent advances in our understanding of telomerase inhibitors, the relationships between telomerase inhibitors, cancer, and fields such as inflammation.


METHODS
This review summarizes new patents published on telomerase inhibitors from 2010 to 2015.


CONCLUSIONS
The review provides a brief account of the background, development, and on-going issues involving telomerase inhibitors. In particular, this review emphasizes imetelstat (GRN163L) and some typical G-quadruplex stabilizers that participate in telomerase inhibition. Overall, the research scope of antineoplastic is becoming broader and telomerase inhibitors have been shown to be a promising therapeutic target. Therefore, novel antineoplastic agents with greater activity and higher specificity must be developed.
a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing , People's Republic of China.|b Preparatory College Education , Guangxi University for Nationalities , Nanning , People's Republic of China.
Ruo-Jun
RJ
Man
a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing , People's Republic of China.
Long-Wang
LW
Chen
a State Key Laboratory of Pharmaceutical Biotechnology , Nanjing University , Nanjing , People's Republic of China.
Hai-Liang
HL
Zhu
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007211:Indoles / Q000494:pharmacology / Q000627:therapeutic use; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D009536:Niacinamide / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D009841:Oligonucleotides; D010330:Patents as Topic; D019098:Telomerase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007211:Indoles; D009841:Oligonucleotides; D009536:Niacinamide; D019098:Telomerase; C519562:imetelstat
Telomere; antineoplastic; diagnostic methods; imetelstat (GRN163L); telomerase; telomerase inhibitor; therapies