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Study on Effects of Molecular Crowding on G-quadruplex-ligand Binding and Ligand-Mediated Telomerase Inhibition

Study on Effects of Molecular Crowding on G-quadruplex-ligand Binding and Ligand-Mediated Telomerase Inhibition

Hidenobu Yaku, Takashi Murashima, Hisae Tateishi-Karimata, Shu-ichi Nakano, Daisuke Miyoshi, Naoki Sugimoto

Methods. 2013 Nov;64(1):19-27.

PMID: 23562626

Abstract:

The telomere G-quadruplex-binding and telomerase-inhibiting capacity of two cationic (TMPyP4 and PIPER) and two anionic (phthalocyanine and Hemin) G-quadruplex-ligands were examined under conditions of molecular crowding (MC). Osmotic experiments showed that binding of the anionic ligands, which bind to G-quadruplex DNA via π-π stacking interactions, caused some water molecules to be released from the G-quadruplex/ligand complex; in contrast, a substantial number of water molecules were taken up upon electrostatic binding of the cationic ligands to G-quadruplex DNA. These behaviors of water molecules maintained or reduced the binding affinity of the anionic and the cationic ligands, respectively, under MC conditions. Consequently, the anionic ligands (phthalocyanine and Hemin) robustly inhibited telomerase activity even with MC; in contrast, the inhibition of telomerase caused by cationic TMPyP4 was drastically reduced by MC. These results allow us to conclude that the binding of G-quadruplex-ligands to G-quadruplex via non-electrostatic interactions is preferable for telomerase inhibition under physiological conditions.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP123439805	Copper phthalocyanine-3,4′,4″,4″′-tetrasulfonic acid tetrasodium salt		123439-80-5	Price
AP215297180	N,N′-Bis[2-(2-tert-butyldimethylsilyloxyethoxy)ethyl]-3,4,9,10-perylenetetracarboxylic diimide		215297-18-0	Price

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