News at CHESS 2004

• CHESS Home
• Archive
• 2004
• 2005
• 2006
• 2007
• 2008

HIV's Crystal Key

Eddy Arnold, Center for Advanced Biotechnology and Medicine and Rutgers University Department of Chemistry and Chemical Biology, was recently featured in the Star-Ledger, December 12, 2004 for his crusading research in the pursuit of revolutionary AIDS drugs (DAPY compounds) which may be more effective treatments for HIV, the deadly virus that causes AIDS.  Through Arnold's crystallography research and dedication to the concept that reverse transcriptase (RT) was a key target of HIV, the future now looks promising with one of the DAPY compounds (TMC-125) entering Phase III clinical trials in the near future.  Arnold's group, which has used CHESS extensively to study RT, continues its efforts to detail the structure and function of RT, and to develop new classes of inhibitors that may be able to more effectively evade HIV drug resistance.  They are also pursuing the development of an AIDS vaccine by generating combinatorial libraries of chimeric human rhinoviruses displaying key HIV neutralizing epitopes, including segments of the HIV-1 gp41, part of the highly conserved viral fusion machinery.

Complete article here (pdf)

To view Arnold's recent publications in the Journal of Medicinal Chemistry, click on the article below (these are links directly to the J. of Medicinal Chemistry and may require a subscription):

In Search of a Novel Anti-HIV Drug: Multidisciplinary Coordination in the Discovery of 4-[[4-[[4-[(1E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile (R278474, Rilpivirine)

Roles of Conformational and Positional Adaptability in Structure-Based Design of TMC125-R165335 (Etravirine) and Related Non-nucleoside Reverse Transcriptase Inhibitors That Are Highly Potent and Effective against Wild-Type and Drug-Resistant HIV-1 Variants

Synthesis of Novel Diarylpyrimidine Analogues and Their Antiviral Activity against Human Immunodeficiency Virus Type 1

Design, Synthesis, and SAR of a Novel Pyrazinone Series with Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitory Activity