Anticancer vaccine: Antigen 2 made out of a tripeptide of β‐D‐Galp‐(1→3)‐CH2‐α‐D‐GalNAc‐O‐Ser and conjugated with keyhole limpet hemocyanin (KLH) protein induced an early and strong immune response (IgG antibodies) in mice. Antigen 3 made out of an α‐C‐galactoside analogue did not induce such an immune response (see scheme).
In
vitro selection technologies are important tools for identifying
high affinity peptides to proteins of broad medical and biological
interest. However, the technological advances that have made it possible
to generate long lists of candidate peptides have far outpaced our
ability to characterize the binding properties of individual peptides.
Here, we describe a low cost strategy to rapidly synthesize, purify,
screen, and characterize peptides for high binding affinity. Peptides
are assayed in a 96-well dot blot apparatus using membranes that enable
partitioning of bound and unbound peptide–protein complexes.
We have validated the binding affinity constants produced by this
method using known peptide ligands and applied this process to discover
five new peptides with nanomolar affinity to human α-thrombin.
Given the need for new analytical tools that can accelerate peptide
discovery and characterization, we feel that this approach would be
useful to a wide range of technologies that utilize high affinity
peptides.
FK866 (also named APO866 or WK175) is a potent NAMPT inhibitor being evaluated (Phase II) as a potential anticancer drug. The preparation of the C‐iminoribofuranoside analog (2E)‐N‐[4‐(1‐benzoylpiperidin‐4‐yl)butyl]‐3‐{3‐[(2S,3S,4R,5R)‐3,4‐dihydroxy‐5‐(hydroxymethyl)pyrrolidin‐2‐yl]phenyl}prop‐2‐enamide ((−)‐1) is reported.
2. Ferrando A, Neuberg D, Dodge RK, et al. Adult T-cell ALL patients whose lymphoblasts express the HOX11 oncogene have an excellent prognosis when treated with chemotherapy and are not candidates for allogeneic bone marrow transplantaton in first remission.
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