The spiropiperidine-3,3′-oxindole scaffold: a type II β-turn peptide isostere
نویسندگان
چکیده
منابع مشابه
the investigation of the relationship between type a and type b personalities and quality of translation
چکیده ندارد.
Angiotensin II analogs comprised of Pro-Amb (γ-turn scaffold) as angiotensin II type 2 (AT(2)) receptor agonists.
We describe herein the design, synthesis and conformational investigation of Pro-Amb (proline-3-amino-2-methoxybenzoic acid) incorporated Angiotensin II and its truncated analogues. Solution-state NMR and CD studies suggest γ-turn-like conformation in Pro-Amb analogs in aqueous solution. Furthermore, Pro-Amb analogs have been shown to act as AT2 receptor agonists.
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Aiming at restricting the conformational freedom of tryptophan-containing peptide ligands, we designed a THBC (tetrahydro-β-carboline)-DKP (diketopiperazine)-based peptidomimetic scaffold capable of arranging in an unusual α-turn conformation. The synthesis is based on a diastereoselective Pictet-Spengler condensation to give the THBC core, followed by an intramolecular lactamization to complet...
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A strategy was developed to extend the lifetime of an peptide-based substrate for Abl kinase in the cytosolic environment. Small β-turn structures were added to the peptide's N-terminus to block entry into peptidase catalytic sites. The influence of the size of the β-turn and two covalent cross-linking strategies on the rate of hydrolysis was assessed. The most peptidase-resistant substrate was...
متن کاملLeft-handed helical preference in an achiral peptide chain is induced by an L-amino acid in an N-terminal type II β-turn.
Oligomers of the achiral amino acid Aib adopt helical conformations in which the screw-sense may be controlled by a single N-terminal residue. Using crystallographic and NMR techniques, we show that the left- or right-handed sense of helical induction arises from the nature of the β-turn at the N terminus: the tertiary amino acid L-Val induces a left-handed type II β-turn in both the solid stat...
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ژورنال
عنوان ژورنال: Tetrahedron
سال: 2010
ISSN: 0040-4020
DOI: 10.1016/j.tet.2010.04.077