Synthesis and properties of PI polyamide–SAHA conjugate
A Ohtsuki, MT Kimura, M Minoshima, T Suzuki… - Tetrahedron …, 2009 - Elsevier
We have designed and synthesized new types of pyrrole (P)-imidazole (I) polyamide
conjugates 1 and 2 possessing a suberoylanilide hydroxamic acid (SAHA) moiety that is a
strong inhibitor of histone deacetylase (HDAC). SAHA conjugate 2 was designed to target
the promoter region of the p16 tumor suppressor gene. The DNA binding affinity of SAHA
conjugate 2 to its target sequence was examined using surface plasmon resonance. HDAC
inhibition activity of conjugates 1 and 2 was evaluated using a colorimetric assay. The …
conjugates 1 and 2 possessing a suberoylanilide hydroxamic acid (SAHA) moiety that is a
strong inhibitor of histone deacetylase (HDAC). SAHA conjugate 2 was designed to target
the promoter region of the p16 tumor suppressor gene. The DNA binding affinity of SAHA
conjugate 2 to its target sequence was examined using surface plasmon resonance. HDAC
inhibition activity of conjugates 1 and 2 was evaluated using a colorimetric assay. The …