Discovery and development of Santacruzamate A, a potent and selective histone deacetylase inhibitor

Researchers discovered santacruzamate A, a potent and selective histone deacetylase (HDAC) inhibitor with picomolar-level inhibition of HDAC2, during an expedition to Coiba National Park, a UNESCO World Heritage Site in Panama. This compound shares structural similarities with Vorinostat®, a clinically approved HDAC inhibitor for treating refractory cutaneous T-cell lymphoma. Bioactivity-guided fractionation led to its isolation from a dark brown cyanobacterium, potentially representing a new genus within marine cyanobacteria. The study also established a robust synthesis method for santacruzamate A and synthesized analogs to further evaluate their biological activity.

Balunas, M., Pavlik, C., Wong, C., Lopez, D., Engene, N., McPhail, K., & Gerwick, W. (2012). Discovery and development of Santacruzamate A, a potent and selective histone deacetylase inhibitor. Planta Medica, 78(11). https://doi.org/10.1055/s-0032-1320261