Serge Bouaziz
Faculté de Pharmacie
Structural and functional studies of new therapeutic targets by NMR
Website: https://www.citcom.cnrs.fr
ORCID: 0000-0001-7792-8307
Structural and functional studies of new therapeutic targets by NMR
My research activity concerns the structural and functional study of new therapeutic targets. My objective is the structural characterization of these targets and their complexes by NMR in order to elucidate their mechanism of recognition and action, to translate these interactions into functional terms and to use these molecules as potential targets for the rational development of new therapeutic ligands. My research projects concern:
(A) HIV-1 proteins as targets (1) mechanism of action of HIV-1 maturation inhibitors, (2) interactions of the HIV-1 Vpr protein with the cellular restriction factor UNG2, with p6 protein and study of its chaperone effect on nucleic acids. (3) Structural studies of complexes between NCp7 and nucleic acids combining NMR and molecular dynamics and between NCp7 and p6, a potential regulator of RNA recognition by NCp7.
(B) Structural studies of the agnoprotein of the human polyomavirus, inhibition of the formation of dimers by mimetic peptides.
(C) Study of the polymerase complex of SARS-CoV-2 aimed at identifying ligands disrupting polymerase complex, activity and viral replication.
(D) Projects in collaboration with chemists: targeting of the VEGF-VEGFR1d2 protein interface, characterization of macrocyclic peptides stabilizing protein α-turns, DNA compaction in thiourea lipids, synthesis and structural studies of a new class of cyclin-dependent kinase inhibitors.
Top 5 publications
1- Chen X, Coric P, Bouaziz S. 1H, 13C and 15N backbone resonance assignment of HIV-1 Gag (276-432) encompassing the C-terminal domain of the capsid protein, the spacer peptide 1 and the nucleocapsid protein. Biomol NMR Assign. 2021 Oct;15(2):267-271. doi: 10.1007/s12104-021-10016-9. Epub 2021 Mar 22. PMID: 33754285.
2- Chen X, Coric P, Larue V, Turcaud S, Wang X, Nonin-Lecomte S, Bouaziz S. The HIV-1 maturation inhibitor, EP39, interferes with the dynamic helix-coil equilibrium of the CA-SP1 junction of Gag. Eur J Med Chem. 2020 Oct 15;204:112634. doi:10.1016/j.ejmech.2020.112634. Epub 2020 Jul 18. PMID: 32717487.
3- Wang X, Chen X, Nonin-Lecomte S, Bouaziz S. Acetonitrile allows indirect replacement of nondeuterated lipid detergents by deuterated lipid detergents for the nuclear magnetic resonance study of detergent-soluble proteins. Protein Sci. 2021 Nov;30(11):2324-2332. doi:10.1002/pro.4174. Epub 2021 Sep 9. PMID: 34462977; PMCID: PMC8521311.
4- Kara H, Chazal N, Bouaziz S. Is Uracil-DNA Glycosylase UNG2 a New Cellular Weapon Against HIV-1? Curr HIV Res. 2019;17(3):148-160. doi: 10.2174/1570162X17666190821154331. PMID: 31433761.
5- Coric P, Saribas AS, Abou-Gharbia M, Childers W, Condra JH, White MK, Safak M, Bouaziz S. Nuclear Magnetic Resonance Structure of the Human Polyoma JC Virus Agnoprotein. J Cell Biochem. 2017 Oct;118(10):3268-3280. doi: 10.1002/jcb.25977. Epub 2017 May 3. PMID: 28295503; PMCID: PMC5550335.
Dernières publications sur HAL :
- [hal-01061760] Targeting the Proangiogenic VEGF-VEGFR Protein-Protein Interface with Drug-like Compounds by In Silico and In...by ano.nymous@ccsd.cnrs.fr.invalid (Benoît Gautier) on 29 May 2024 at 23h35
Protein-protein interactions play a central role in medicine, and their modulation with small organic compounds remains an enormous challenge. […]
- [hal-02122333] Accurate nanoscale flexibility measurement of DNA and DNA–protein complexes by atomic force microscopy in liquidby ano.nymous@ccsd.cnrs.fr.invalid (Divakaran Murugesapillai) on 30 January 2024 at 10h50
The elasticity of double-stranded DNA (dsDNA), as described by its persistence length, is critical for many biological processes, including genomic […]
- [hal-02122318] Expression of novel proteins by polyomaviruses and recent advances in the structural and functional features of...by ano.nymous@ccsd.cnrs.fr.invalid (A. Sami Saribas) on 30 January 2024 at 10h49
Polyomavirus family consists of a highly diverse group of small DNA viruses. The founding family member (MPyV) was first discovered in the newborn […]
- [hal-02460685] Emerging From the Unknown: Structural and Functional Features of Agnoprotein of Polyomavirusesby ano.nymous@ccsd.cnrs.fr.invalid (A. Sami Saribas) on 30 January 2024 at 10h49
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