Structure-activity relationships of cyclic and linear peptide T analogues.
Using the potent cyclic peptide T analog [formula: see text] as parent compound, a series of analogues were synthesized and their potencies in a monocyte chemotaxis assay were compared with those of correspondingly modified linear peptides. Structure-activity relationships observed with cyclic compounds did not always parallel those determined with linear analogues. [formula: see text] showed the highest affinity to CD4 receptor of monocytes of any peptide thus far studied. It also proved to be highly resistant to degradation by plasma or brain enzymes.
Marastoni
M
M
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Salvadori
S
S
Balboni
G
G
Scaranari
V
V
Spisani
S
S
Reali
E
E
Traniello
S
S
Tomatis
R
R
D000595:Amino Acid Sequence; D001769:Blood / Q000378:metabolism; D001921:Brain / Q000378:metabolism; D015704:CD4 Antigens / Q000378:metabolism; D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008969:Molecular Sequence Data; D009000:Monocytes / Q000187:drug effects; D015717:Peptide T / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D015704:CD4 Antigens; D010456:Peptides, Cyclic; D015717:Peptide T