Protein Information

Name Telomerase (protein family or complex)
Synonyms Telomerase; Telomerases

Compound Information

Name anthraquinone
CAS 9,10-anthracenedione

Reference List

PubMed Abstract RScore(About this table)
18571928 Huang HS, Huang KF, Li CL, Huang YY, Chiang YH, Huang FC, Lin JJ: Synthesis, human telomerase inhibition and anti-proliferative studies of a series of 2,7-bis-substituted amido-anthraquinone derivatives. Bioorg Med Chem. 2008 Jul 15;16(14):6976-86. Epub 2008 Jun 2.
88(1,1,1,8) Details
10411488 Perry PJ, Read MA, Davies RT, Gowan SM, Reszka AP, Wood AA, Kelland LR, Neidle S: 2,7-Disubstituted amidofluorenone derivatives as inhibitors of human telomerase. J Med Chem. 1999 Jul 15;42(14):2679-84.

We have previously identified anthraquinone-based molecules capable of inhibiting telomerase by stabilizing G-quadruplex structures formed by the folding of telomeric DNA.
84(1,1,1,4) Details
11814869 Cairns D, Michalitsi E, Jenkins TC, Mackay SP: Molecular modelling and cytotoxicity of substituted anthraquinones as inhibitors of human telomerase. Bioorg Med Chem. 2002 Mar;10(3):803-7.

Molecular modelling has been carried out for a number of amine-functionalised anthraquinone derivatives to determine their extent of binding to G-tetraplex DNA and their ability to inhibit the enzymes telomerase and Taq polymerase.
163(2,2,2,3) Details
18754611 Zagotto G, Sissi C, Lucatello L, Pivetta C, Cadamuro SA, Fox KR, Neidle S, Palumbo M: Aminoacyl-anthraquinone conjugates as telomerase inhibitors: synthesis, biophysical and biological evaluation. J Med Chem. 2008 Sep 25;51(18):5566-74.
64(0,2,2,4) Details
15698759 Huang HS, Chou CL, Guo CL, Yuan CL, Lu YC, Shieh FY, Lin JJ: Human telomerase inhibition and cytotoxicity of regioisomeric disubstituted amidoanthraquinones and aminoanthraquinones. Bioorg Med Chem. 2005 Mar 1;13(5):1435-44.

The present study details the effects on human telomerase of these new classes of 1,4- and 1,5-difunctionalized tricyclic anthraquinone compounds.
11(0,0,1,6) Details
17268103 Huang HS, Chen IB, Huang KF, Lu WC, Shieh FY, Huang YY, Huang FC, Lin JJ: Synthesis and human telomerase inhibition of a series of regioisomeric disubstituted amidoanthraquinones. Chem Pharm Bull. 2007 Feb;55(2):284-92.

These results greatly expand the potential of tricyclic anthraquinone pharmacophore in preventive and/or curative therapy.
9(0,0,0,9) Details
17936629 Zagotto G, Sissi C, Moro S, Dal Ben D, Parkinson GN, Fox KR, Neidle S, Palumbo M: Amide bond direction modulates G-quadruplex recognition and telomerase inhibition by 2,6 and 2,7 bis-substituted anthracenedione derivatives. Bioorg Med Chem. 2008 Jan 1;16(1):354-61. Epub 2007 Sep 25.

To understand the basis of amido anthracenedione selectivity, we have synthesized a number of derivatives bearing the -CO-NH- or -NH-CO- group linked to the planar anthraquinone (AQ) moiety at 2,6 and 2,7 positions.
5(0,0,0,5) Details
12852760 Huang HS, Chiou JF, Fong Y, Hou CC, Lu YC, Wang JY, Shih JW, Pan YR, Lin JJ: Activation of human telomerase reverse transcriptase expression by some new symmetrical bis-substituted derivatives of the anthraquinone. J Med Chem. 2003 Jul 17;46(15):3300-7.

Since the telomerase enzyme is a novel target for potential anticancer therapy and stem cell expansion, we explore the biological effects of these compounds by evaluating their effects on telomerase activity and telomerase expression.
2(0,0,0,2) Details
15519160 Huang HS, Chiu HF, Lee AL, Guo CL, Yuan CL: Synthesis and structure-activity correlations of the cytotoxic bifunctional 1,4-diamidoanthraquinone derivatives. Bioorg Med Chem. 2004 Dec 1;12(23):6163-70.

Anthraquinone-based compounds are attractive target for the design of new anticancer drugs.
We have previously described a series of 1,5- and 1,4-difunctionalized anthraquinones, which exhibit different spectra of potency, together with human telomerase evaluation.
1(0,0,0,1) Details
15638760 Kubin A, Wierrani F, Burner U, Alth G, Grunberger W: Hypericin--the facts about a controversial agent. Curr Pharm Des. 2005;11(2):233-53.

John's Wort (Hypericum species) and can also be synthesized from the anthraquinone derivative emodin.
In other contemporary studies, screening hypericin for inhibitory effects on various pharmaceutically important enzymes such as MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450), has yielded results supporting therapeutic potential.
1(0,0,0,1) Details