Research Areas

 

   

Interaction of nucleosomes with small synthetic molecules and with transcription factors

Nucleosomal DNA is highly distorted and partially occluded from the solvent due to its tight interaction with the histone octamer. Thus, nucleosome architecture greatly affects the accessibility of nucleosomal DNA for global and specific regulators. We are investigating recognition of nucleosomes by small molecules, viral proteins, and transcriptional regulators, using fluorescence anisotropy, fluorescence resonance energy transfer, analytical ultracentrifugation, gel electrophoresis, and x-ray crystallography. In particular, we are interested to what degree nucleosome structure adjusts to better accommodate interacting factors.

Pyrole-imidazole polyamide clampIn collaboration with the Dervan and Gottesfeld laboratories, we have demonstrated that nucleosomal DNA is quite accessible for molecular recognition. Pyrrole-imidazole polyamides bind nucleosomal DNA with high affinity and specificity, and evoke distinct structural changes in nucleosomal DNA. These results demonstrate that nucleosomal DNA is capable of adjusting (within limits) to provide an optimal binding environment for a ligand while still remaining tightly bound to the histone octamer. We have further shown that polyamides that bind nucleosomal DNA severely limit the ability of the histone octamer to reposition with respect to the DNA, thereby completely inhibiting in vitro transcription.

We have recently expanded our studies to protein transcription factors. Using a combination of methods, most notably x-ray crystallography, and fluorescence resonance energy transfer between defined regions within the nucleosome, we investigate the structural changes that are inflicted upon the nucleosome and the transcription factor as a consequence of binding to nucleosomal DNA. Effects on higher order structure are also studied using analytical ultracentrifugation and atomic force microscopy.
 
We are also investigating how the nucleosomal surface may serve as a binding platform for cellular and viral factors. We have started by studying how Kaposi’s sarcoma herpes virus protein LANA enables the viral genome to tether onto chromosomes so that virus is not lost from cells. The mechanism by which LANA latches onto chromosomes was previously unknown. We have found that LANA engages histones H2A and H2B to dock onto chromosomes by binding to the nucleosomal surface via a tight hairpin motif. This study (which is the result of an on-going collaboration with Dr. Kenneth Kaye) unequivocally demonstrates how a highly structured nucleosomal surface acts as an interaction platform for molecular recognition.

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LANA peptide bound to nucleosome
LANA peptide bound to a nucleosome

 

Pyrole-imidazole polyamides gel
Pyrrole-imidazole polyamides stabilize nucleosomes (PNAS 101, 6864-9, 2004)