745821-84-5Relevant articles and documents
Privileged scaffolds for blocking protein-protein interactions: 1,4-Disubstituted naphthalene antagonists of transcription factor complex HOX-PBX/DNA
Ji, Tao,Lee, Madison,Pruitt, Steven C.,Hangauer, David G.
, p. 3875 - 3879 (2004)
Structure-based-design studies, with the crystal structure of the HOXB1-PBX1/DNA transcription factor complex, were used to identify 1,4-disubstituted naphthalenes as potential antagonists. An initial library of 32 analogs was synthesized, two of which were found to be more potent than the reported activity for a 12 amino acid peptide antagonist. Antagonists were also identified of the related BRN1/DNA and BRN2/DNA transcription factor complexes indicating that a 1,4-disubsituted naphthalene may be a privileged scaffold for preparing screening libraries targeting this family of transcription factor complexes.
