One bead, one chemical compound: Use of the selectide process for anticancer drug discovery

Sydney E. Salmon, Kit Lam, Stephen Felder, Helen Yeoman, Joseph Schlessinger, Axel Ullrich, Viktor Krchnák, Michael Lebl

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

A technology for chemical synthesis and testing of libraries of millions of chemical entities has been developed for rapid molecular and cellular screening for drug leads. Each individual compound in the library is on a separate resin bead. Screening for binding activity can be conducted directly on the beads. Biological activity is assessed in solution phase assay by cleaving a portion of the compound from each bead. The molecular structure of the compound of interest is obtained by automated peptide sequencing from the bead of origin. We have applied this technology to anticancer drug discovery as well as to other pharmaceutical targets. For anticancer drug development, current molecular targets include B-cell lymphoma, the EGF receptor, and the HER2-neu receptor. Solution phase screening with dual cleavable libraries is being used for growth inhibition of human tumor cell lines. Initial in vitro leads have been identified in each of these areas of anticancer drug discovery.

Original languageEnglish (US)
Pages (from-to)127-131
Number of pages5
JournalActa Oncologica
Volume33
Issue number2
DOIs
StatePublished - 1994
Externally publishedYes

Fingerprint

Drug Discovery
Libraries
ErbB-2 Receptor
Small Molecule Libraries
Technology
Preclinical Drug Evaluations
B-Cell Lymphoma
Molecular Structure
Tumor Cell Line
Epidermal Growth Factor Receptor
Pharmaceutical Preparations
Peptides
Growth
In Vitro Techniques

ASJC Scopus subject areas

  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Hematology

Cite this

Salmon, S. E., Lam, K., Felder, S., Yeoman, H., Schlessinger, J., Ullrich, A., ... Lebl, M. (1994). One bead, one chemical compound: Use of the selectide process for anticancer drug discovery. Acta Oncologica, 33(2), 127-131. https://doi.org/10.3109/02841869409098395

One bead, one chemical compound : Use of the selectide process for anticancer drug discovery. / Salmon, Sydney E.; Lam, Kit; Felder, Stephen; Yeoman, Helen; Schlessinger, Joseph; Ullrich, Axel; Krchnák, Viktor; Lebl, Michael.

In: Acta Oncologica, Vol. 33, No. 2, 1994, p. 127-131.

Research output: Contribution to journalArticle

Salmon, SE, Lam, K, Felder, S, Yeoman, H, Schlessinger, J, Ullrich, A, Krchnák, V & Lebl, M 1994, 'One bead, one chemical compound: Use of the selectide process for anticancer drug discovery', Acta Oncologica, vol. 33, no. 2, pp. 127-131. https://doi.org/10.3109/02841869409098395
Salmon, Sydney E. ; Lam, Kit ; Felder, Stephen ; Yeoman, Helen ; Schlessinger, Joseph ; Ullrich, Axel ; Krchnák, Viktor ; Lebl, Michael. / One bead, one chemical compound : Use of the selectide process for anticancer drug discovery. In: Acta Oncologica. 1994 ; Vol. 33, No. 2. pp. 127-131.
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