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NUCLEOTIDE INTERACTING LIBS

 

Topoisomerase II residues 409-1201 / NMR Structure of a 21 bp DNA duplex preferentially cleaved by

Human Topoisomerase II (10 conformations) / Structure of the Topoisomerase II poison bound to DNA

Nucleotides are the basic components of nucleic acids, including DNA and RNA. They are built on the association of a base, a sugar and phosphates. Combining five nitrogenous bases (A, C, G, T and U), two sugars (ribose and 2’-deoxyribose) and one to three phosphate groups leads to a large diversity of nucleic acids involved in many biological processes, as gene transmission.

Many mutagens fit into the space between two adjacent base pairs (intercalating agents). Most of these molecules are aromatic and planar and their presence prevents DNA to adopt its double helix structure, inhibiting transcription and replication, causing toxicity and mutations. These toxins can be used for therapeutic purposes in chemotherapy to stop the growing of cancer cells.

Many proteins have to recognize nucleotides during their biological action and have a specific site dedicated to this. Among others, kinases, phosphodiesterases, polymerases, reverse transcriptases and topoisomerases belong to this category. Nucleotide interacting molecules can block the function of these proteins in order to have an action on a specific biological pathway.

AMINOPYRAZOLE LIBRARY
AMINOPYRAZOLE LIBRARY

• privileged structures for interacting with nucleotidic sites of enzymes: kinases, phosphodiesterases, reverse transcriptases
• focused library with low molecular weight compounds and high diversity
• pharmacophoric pattern also present in GPCR and ion channel ligands
• drug-like structure of special interest for anti-cancer, anti-viral and anti-bacterial leads with oral activity described for some analogues
• library based on 24 intermediates

BENZIMIDAZOLE LIBRARY
BENZIMIDAZOLE LIBRARY

• privileged scaffold interacting with nucleotidic structures, nucleotidic processing enzymes and tubulin
• drug-like structures of special interest for anti-cancer, anti-parasitic and anti-bacterial leads
• focused library with low molecular weight
• systematic variations enabling preliminary SAR establishment
• library based on 24 intermediates

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