A “cross-stitched” peptide with improved helicity and proteolytic stability†
Thomas E.
Speltz, 
‡a
Christopher G.
Mayne,
‡bd
Sean W.
Fanning,
c
Zamia
Siddiqui,
a
Emad
Tajkhorshid,
b
Geoffrey L.
Greene
c
and
Terry W.
Moore
*a
‡a
Christopher G.
Mayne,
‡bd
Sean W.
Fanning,
c
Zamia
Siddiqui,
a
Emad
Tajkhorshid,
b
Geoffrey L.
Greene
c
and
Terry W.
Moore
*a
Abstract
A new computational approach to obtain quantitative energy profiles for helix folding was used in the design of orthogonal hydrocarbon and lactam bicyclic peptides. The proteolytically stable, “cross-stitched” peptide SRC2-BCP1 shows nanomolar affinity for estrogen receptor α and X-ray crystallography confirms a helical binding pose.
- This article is part of the themed collection: Mechanistic, computational & physical organic chemistry in OBC
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