News Releases & Research Results Hybrid compounds of small molecule CD4 mimics and polyethylene glycol units as HIV entry inhibitors - Combined therapy with an antibody for radical care -

The results of collaborative research led by Professor Hirokazu Tamamura of the Department of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Professor Shuzo Matsushita of The Joint Research Center for Human Retrovirus Infection, Kumamoto University, Associate Professor Tomoyuki Miura of the Institute for Frontier Life and Medical Sciences, Kyoto University, Senior Researcher Shigeyoshi Harada of the AIDS Research Center, National Institute of Infectious Diseases, and Director Kazuhisa Yoshimura of the Institute of Public Health, Bureau of Social Welfare and Public Health, Tokyo Metropolitan Government.

• Low-molecular-weight compounds called “CD4 mimics,” which have been investigated for many years, were attached to polyethylene glycol (PEG) units, thereby improving anti-human immunodeficiency virus (HIV) activity, reducing cytotoxicity, and improving pharmacokinetics in a rhesus macaque.
• The development of novel anti-AIDS drugs can be expected with marked effects in combination with an HIV neutralizing antibody.
• The results of this research should apply to the development of therapeutic methods with few side effects for radical cure in combination with antibodies.

This project was conducted with the support of the Research Program on HIV/AIDS by AMED.

The results were published online in Journal of Medicinal Chemistry on January 27.

Kobayakawa T., et al. Hybrids of Small-Molecule CD4 Mimics with Polyethylene Glycol Units as HIV Entry Inhibitors Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.0c01153