The structural basis of homo- and heterodimerization of two chemokine receptors: Implications in HIV-1 cell entry

NIH RePORTER · NIH · R56 · $758,083 · view on reporter.nih.gov ↗

Abstract

SUMMARY The chemokine receptors CCR5 and CXCR4 play essential roles in the human immune system and are involved in HIV infection and cancer metastasis. Several studies have demonstrated the role of homo- and heterodimerization of these receptors in modulating protein function by affecting their chemokine sensitivity or altering their G protein coupling mechanisms. Moreover, the ability of HIV to infect T cells utilizing either CXCR4 or CCR5 as a co-receptor has been shown to depend on homo- and heterodimerization. Consequently, the association of these two chemokine receptors has increasingly gained attention for drug design. At this time, there is no high-resolution structure available for CCR5 or CXCR4 homo- or heterodimers due to the complexity of the crystallization and sample preparation for EM. In aim 1, we will study the dimerization of CCR5 protein at both molecular and functional levels. In aim 2, we will study the heterodimerization of CCR5 and CXCR4. In aim 3, we will develop a nanodisc-based fusion assay. Moreover, we will image HIV pseudovirus particles binding and fusion with large nanodiscs containing CD4/CCR5 or CD4/CXCR4.

Key facts

NIH application ID
10455267
Project number
1R56AI150406-01A1
Recipient
BRIGHAM AND WOMEN'S HOSPITAL
Principal Investigator
Mahmoud Nasr
Activity code
R56
Funding institute
NIH
Fiscal year
2021
Award amount
$758,083
Award type
1
Project period
2021-08-20 → 2023-01-31