Convergent diversity-oriented side-chain macrocyclization scan for unprotected polypeptides

Convergent diversity-oriented side-chain macrocyclization scan for unprotected polypeptides.

Here we describe a general synthetic platform for side-chain macrocyclization of an unprotected peptide library based on the SNAr reaction between cysteine thiolates and a new generation of highly reactive perfluoroaromatic small molecule linkers. This strategy enabled us to simultaneously "scan" two cysteine residues positioned from i, i + 1 to i, i + 14 sites in a polypeptide, producing 98 ma...

Enzyme-Catalyzed Macrocyclization of Long Unprotected Peptides

A glutathione S-transferase (GST) catalyzed macrocyclization reaction for peptides up to 40 amino acids in length is reported. GST catalyzes the selective S(N)Ar reaction between an N-terminal glutathione (GSH, γ-Glu-Cys-Gly) tag and a C-terminal perfluoroaryl-modified cysteine on the same polypeptide chain. Cyclic peptides ranging from 9 to 24 residues were quantitatively produced within 2 h i...

Convergent diversity-oriented synthesis of small-molecule hybrids.

Synthesis-for-scan and scan chain ordering

Designing a testable circuit is often a two step process. First, the circuit is designed to conform to the functional specifications. Then, the testability aspects are added. By taking the test strategy into account during the synthesis of the circuit, the overhead due to the test features can be reduced. We present a synthesis-for-scan procedure, called beneficial scan, that orders the scan ch...

Side-scan Sonar for Inspecting Coastal Structures

INTRODUCTION: SSS has been used to map the sea bottom and search for submerged objects since the 1960's (Fleming, 1976). Recent experiments by CERC and the Buffalo District have shown SSS to be useful for inspecting both sloping coastal structures (i.e., rubble-mound jetties and breakwaters) and vertical-wall structures (i.e., concrete caissons and timber cribs). SSS is an adaptation of high-fr...