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Biophysical Screens Identify Fragments That Bind to the Viral DNA-Binding Proteins EBNA1 and LANA
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Biophysical Screens Identify Fragments That Bind to the Viral DNA-Binding Proteins EBNA1 and LANA
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Journal Article
Biophysical Screens Identify Fragments That Bind to the Viral DNA-Binding Proteins EBNA1 and LANA
2020
Overview
The human gamma-herpesviruses Epstein–Barr virus (EBV) (HHV-4) and Kaposi’s sarcoma-associated herpesvirus (KSHV) (HHV-8) are responsible for a number of diseases, including various types of cancer. Epstein–Barr nuclear antigen 1 (EBNA1) from EBV and latency-associated nuclear antigen (LANA) from KSHV are viral-encoded DNA-binding proteins that are essential for the replication and maintenance of their respective viral genomes during latent, oncogenic infection. As such, EBNA1 and LANA are attractive targets for the development of small-molecule inhibitors. To this end, we performed a biophysical screen of EBNA1 and LANA using a fragment library by saturation transfer difference (STD)–NMR spectroscopy and surface plasmon resonance (SPR). We identified and validated a number of unique fragment hits that bind to EBNA1 or LANA. We also determined the high-resolution crystal structure of one fragment bound to EBNA1. Results from this screening cascade provide new chemical starting points for the further development of potent inhibitors for this class of viral proteins.
Publisher
MDPI AG,MDPI
Subject
/ Antigens, Viral - metabolism
/ Disease
/ DNA
/ DNA-Binding Proteins - chemistry
/ DNA-Binding Proteins - metabolism
/ Epstein-Barr Virus Nuclear Antigens - chemistry
/ Epstein-Barr Virus Nuclear Antigens - metabolism
/ Epstein–Barr nuclear antigen 1
/ fragment-based lead discovery
/ Herpesvirus 8, Human - metabolism
/ Humans
/ Kaposi’s sarcoma associated herpesvirus (KSHV)
/ latency-associated nuclear antigen
/ Ligands
/ Lymphoma
/ Magnetic Resonance Spectroscopy
/ Nuclear Proteins - chemistry
/ Nuclear Proteins - metabolism
/ Proteins
/ saturation transfer difference-nuclear magnetic resonance
