Peptidomimetic inhibitors targeting the CCR5-binding site on the human immunodeficiency virus type-1 gp120 glycoprotein complexed to CD4.
A helical tyrosine-sulfated epitope in CCR5 that is recognized by the human immunodeficiency virus type-1 envelope glycoprotein gp120 in its CD4-induced conformation can be mimicked structurally by a cyclic β-hairpin peptide containing two sulfated tyrosine residues at positions i and i + 2 along one β-strand.
Seitz
Markus
M
Department of Chemistry, University of Zurich, Winterthurerstrasse 190, 8057 Zurich X, Switzerland.
Rusert
Peter
P
Moehle
Kerstin
K
Trkola
Alexandra
A
Robinson
John A
JA
D001665:Binding Sites / Q000187:drug effects; D001667:Binding, Competitive / Q000187:drug effects; D015704:CD4 Antigens / Q000378:metabolism*; D015699:HIV Envelope Protein gp120 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D018259:Herpesvirus 1, Human; D006801:Humans; D008958:Models, Molecular; D010456:Peptides, Cyclic / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D057786:Peptidomimetics / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D017433:Protein Structure, Secondary; D019713:Receptors, CCR5 / Q000737:chemistry / Q000378:metabolism*
D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D010456:Peptides, Cyclic; D057786:Peptidomimetics; D019713:Receptors, CCR5; C514793:gp120 protein, Human immunodeficiency virus 1