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Synthesis and screening of a cyclic peptide library: Discovery of small-molecule ligands against human prolactin receptor by Tao Liu; Sang Hoon Joo; Jeffrey L. Voorhees; Charles L. Brooks; Dehua Pei is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Synthesis and screening of a cyclic peptide library: Discovery of small-molecule ligands against human prolactin receptor about?

Prolactin receptor is involved in normal lactation and reproduction; however, excessive prolactin levels can cause various reproductive disorders such as prolactinomas. Small-molecule antagonists against the human prolactin receptor (hPRLr) thus have potential clinical applications and may serve as useful molecular probes in biomedical research. In this work, we synthesized a large, support-bound cyclic peptide library (theoretical diversity of 1.2 • 10 7 ) on 90-lm TentaGel beads and screened it against the extracellular domain of hPRLr. To facilitate hit identification, each TentaGel bead was spatially segregated into outer and inner layers, with a cyclic peptide displayed on the bead surface while the bead interior contained the corresponding linear peptide. The identity of a positive bead was revealed by sequencing the linear encoding peptide within the bead by partial Edman degradation/mass spectrometry. Screening of the library resulted in 20 hits, two of which were selected for further analysis and shown to bind to hPRLr with dissociation constants of 2-3 lM.

Who reads Synthesis and screening of a cyclic peptide library: Discovery of small-molecule ligands against human prolactin receptor?

Author

Tao Liu; Sang Hoon Joo; Jeffrey L. Voorhees; Charles L. Brooks; Dehua Pei

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)