Intro
Preface
Acknowledgments
Contents
1: Virus Entry Inhibitors: Past, Present, and Future
1.1 Introduction
1.2 Peptide-Based Virus Entry Inhibitors
1.2.1 Viral Fusion Protein Targeting
1.2.2 Host Protein or Pathway Targeting
1.2.3 The Future of Peptide-Based Virus Entry Inhibitors
1.3 Small-Molecule-Based Virus Entry Inhibitors
1.3.1 Viral Fusion Protein Targeting
1.3.2 Host Protein or Pathway Targeting
1.3.3 The Future of Small-Molecule-Based Virus Entry Inhibitors
1.4 Protein-Based Virus Entry Inhibitors
1.4.1 Viral Fusion Protein Targeting

1.4.2 Host Protein or Pathway Targeting
1.4.3 The Future of Protein-Based Virus Entry Inhibitors
1.5 Conclusion and Prospect
References
2: Peptide-Based HIV Entry Inhibitors
2.1 Introduction
2.2 Peptides Targeting Cellular Receptors
2.3 Peptides Targeting Virus
2.3.1 Peptides Targeting CD4-Binding Site (CD4bs) or Co-Receptor-Binding Site (CoRbs) in the HIV-1 gp120
2.3.2 Peptides Inactivating Cell-Free Virions
2.4 Peptides Blocking Virus-Cell or Cell-Cell Fusion
2.4.1 Peptides Targeting Fusion Peptide (FP) in gp41

2.4.2 Peptide Blocking Six-Helix Bundle (6-HB) Formation
2.4.3 Peptides Targeting the Disulfide Loop Region of gp41
2.5 Conclusion
References
3: Small-Molecule HIV Entry Inhibitors Targeting gp120 and gp41
3.1 Structure and Function of gp120 and gp41
3.2 Small-Molecule HIV-1 Entry Inhibitors Targeting gp120
3.2.1 NBD-556 and Analogs
3.2.2 CD4 Mimics Binding Competitively with gp120 Suppress the Binding of gp120 to CD4
3.2.3 The Acylhydrazone-Containing Small Molecule 18A
3.3 Small-Molecule HIV Entry Inhibitors Target gp41
3.3.1 ADS-J1 and Its Resistance Profile

3.3.2 NB-2, NB-64, A12, GLS-22, and Analogs
3.3.3 NB-206, 12m and Analogs
3.3.4 Indole-Based Compounds, as Small-Molecule HIV-1 Fusion Inhibitors Targeting gp41, Identified
3.3.5 5M038, 5M041 and Analogs Identified by Fluorescence Polarization Assay Using gp41-5 as the Target
3.3.6 Alpha-Helical Mimicry and Colorimetric, Affinity-Based Selection Assay
3.3.7 Natural Polyanionic Ingredient
3.4 Future of HIV-1 Small-Molecule Entry/Fusion Inhibitors and Screening Assay
References
4: The Genesis and Future Prospects of Small Molecule HIV-1 Attachment Inhibitors

4.1 Introduction
4.2 Discovery and SAR of Fostemsavir-Related Series (BMS Series)
4.3 Alternate Chemotypes for Targeting gp120 Unrelated to Keto Amides
4.4 Application of HIV gp120 Inhibitors
4.4.1 As Microbicides
4.4.2 As Target Recognition Element in Conjugates
4.4.3 As Immuno-Protectants or Immuno-Stimulators
4.4.4 As Agents Against Cytopathic and Non-cytopathic Effects of gp120
4.5 Future Directions
4.6 Conclusions
References
5: Endogenous Peptide Inhibitors of HIV Entry
5.1 Introduction
5.2 Antiviral Host Defense Peptides
5.2.1 Defensins