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US 2014/0273278 A1Published application
G-quadruplex binding assays and compounds therefor
OwnerLesley Davenportinventor
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Abstract
The present invention provides methods for assaying binding of compounds to G-quadruplex structures. Also provided are methods for screening candidate compounds for use as modulators of G-quadruplex activity, and methods for screening candidate compounds for telomerase inhibitory activity. The invention further provides novel compounds useful in the assays of the invention.
Claims31
A G-quadruplex analog polynucleotide comprising the structure:
- (5′-(L1)q(L2)r(L3)s(L4)t(L5)u(L6)v)x
- wherein:
- each L1, L2, L3, L4, L5 and L6 is independently selected from the group consisting of a nucleotide, a nucleotide analog, and a nucleotide comprising a 6-methyl-isoxanthopterin nucleobase;
- q, r, s, t, u and v are each independently 0, 1 or 2, provided that the sum of q+r+s+t+u+v is at least 3;
- and
- x is 1 to 8;
- provided that:
- said sequence 5′-(L1)q(L2)r(L3)s(L4)t(L5)u(L6)v is an analog of a telomeric repeat sequence;
- said polynucleotide contains at least one nucleotide comprising a 6-methyl-isoxanthopterin nucleobase;
- said G-quadruplex analog polynucleotide forms or is capable of forming a G-quadruplex structure;
- each 6-methyl-isoxanthopterin nucleobase is located within said G-quadruplex structure;
- the G1 position of said G-quadruplex analog comprises a 6-methyl-isoxanthopterin nucleobase;
- and
- the 6-methyl-isoxanthopterin at said G1 position shows an increase or enhancement in fluorescence upon G-quadruplex formation.
11 more elements
Dependencies are inferred from the claim text.