Biaryl polyamides as a new class of DNA quadruplex-binding ligands.
نویسندگان
چکیده
We report a novel class of biaryl polyamides highly selective for G-quadruplex DNA, and with significant cytotoxicity in several cancer cell lines; they form planar U-shaped structures that match the surface area dimensions of a terminal G-quartet in quadruplex structures rather than the grooves of duplex DNA.
منابع مشابه
Discovery of G-quadruplex stabilizing ligands through direct ELISA of a one-bead-one-compound library.
We describe the identification of small-molecule G-quadruplex ligands using a direct ELISA screen of a one-bead-one-compound library of unnatural polyamides displayed on a branched linker with a biotin tag. This general purpose parallel screen for small molecule-oligonucleotide interactions was validated by surface plasmon resonance and ELISA of resynthesized compounds. Linear polyamides displa...
متن کاملImpact of planarity of unfused aromatic molecules on G-quadruplex binding: learning from isaindigotone derivatives.
G-quadruplex structures are a new class of attractive targets for DNA-interactive anticancer agents. The primary building block of this structure is the G-quartet, which is composed of four coplanar guanines and serves as the major binding site for small molecules. NMR studies and molecular dynamics simulations have suggested that the planarity of G-quartet surface has been highly dynamic in so...
متن کاملMolecular docking based screening of triterpenoids as potential G-quadruplex stabilizing ligands with anti-cancer activity
Triterpenoids isolated from Ganoderma lucidum (GLTs) exhibit a broad spectrum of anti-cancer properties, including anti-proliferative, anti-metastatic and anti-angiogenic activities. Current research studies revealed the role by GLTs in inducing apoptosis and suppression of telomerase activity of cancer cells with much lower toxicity to healthy cells. Compounds selectively binding and stabilizi...
متن کاملCu(II) and Zn(II) complexes with unsymmetrical tetradentate Schiff base ligands: Synthesis, spectral characterization, antimicrobial assay and DNA binding property
The reaction of copper(II) chloride and zinc(II) chloride with N-(2-methylphenyl)-3-(1'-salicylaldehydene-2'-imine-ethane)-butanamide(H2L2a) or (MPSB), N-(2-methylphenyl)-3-(1'-(3'-methoxysalicylaldehydene-2'-imine-ethane)-butanamide (H2L2b) or (MPMSB) and N-(2-methylphenyl)-3-(1'-(2'-hydroxyacetylene-2'-imine-ethane)-butanamide (H2L2c) (MPHB) leads to the formation of a series of new complexes...
متن کاملImportance of minor groove binding zinc fingers within the transcription factor IIIA-DNA complex.
The gene-specific transcription factor IIIA (TFIIIA) binds to the internal promoter element of the 5 S rRNA gene through nine zinc fingers which make specific DNA contacts. Seven of the nine TFIIIA zinc fingers participate in major groove DNA contacts while two fingers, 4 and 6, have been proposed to bind in or across the minor groove. Pyrrole-imidazole polyamides are minor groove binding ligan...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Chemical communications
دوره 27 شماره
صفحات -
تاریخ انتشار 2009