A5067970853- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Carbohydrate Chemistry and Synthesis
- Antimicrobial Peptides and Activities
- Advanced biosensing and bioanalysis techniques
- Innovative Microfluidic and Catalytic Techniques Innovation
- Monoclonal and Polyclonal Antibodies Research
- Microbial Natural Products and Biosynthesis
- Crystallography and molecular interactions
- Biochemical and Structural Characterization
- Synthesis and biological activity
- Organic Chemistry Cycloaddition Reactions
- Blood Coagulation and Thrombosis Mechanisms
- Molecular spectroscopy and chirality
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Catalytic Reactions
- Supramolecular Self-Assembly in Materials
- Fungal Plant Pathogen Control
- Synthesis of Organic Compounds
École Polytechnique Fédérale de Lausanne
2016-2021
Charles Humbert 8
2020
National Chemical Laboratory
2008-2016
Savitribai Phule Pune University
2016
Leipzig University
2008
Durham University
2008
This article describes novel conformationally ordered α/β-hybrid peptides consisting of repeating l-proline-anthranilic acid building blocks. These oligomers adopt a compact, right-handed helical architecture determined by the intrinsic conformational preferences individual amino residues. The striking feature these is their ability to display an unusual periodic pseudo β-turn network nine-membered hydrogen-bonded rings formed in forward direction sequence 1→2 interactions both solid-state...
An efficient cyclization reaction allows for screening of large macrocycle libraries and yields a potent thrombin inhibitor.
Strikingly dissimilar hydrogen-bonding patterns have been observed for two sets of closely similar hetero foldamers containing carboxamide and sulfonamides at regular intervals. Although both maintain conformational ordering, the pattern backbone helical handedness differ diametrically.
Two polar hinges for cyclization of peptides have been developed, leading to bicyclic and cyclized with improved solubility biological activity. Increasingly, we note that a good aqueous is an absolute prerequisite, not only allow handling purification our target but also being crucial activity characteristics. Compared earlier hinges, the 1,1',1"-(1,3,5-triazinane-1,3,5-triyl)tris(2-bromoethanone) (TATB) 2,4,6-tris(bromomethyl)-s-triazine (TBMT), each containing three nitrogen atoms are...
Abstract This article details the characteristic conformational features of Ant‐Pro reverse turn ― a folded pseudo β‐turn motif that displays closed nine‐membered‐ring hydrogen‐bonded network involving just two amino acid residues, namely anthranilic (Ant; constrained β‐amino acid), and proline (Pro; α‐amino acid). The results from extensive investigation ten crystal structures their NMR conformations in solution state provide clear idea about characteristics turn. Ant Pro which form...
Orthanilic acid (2-aminobenzenesulfonic acid, SAnt), an aromatic β-amino has been shown to be highly useful in inducing a folded conformation peptides. When incorporated into peptide sequences (Xaa-SAnt-Yaa), this rigid strongly imparts reverse-turn the backbone, featuring robust 11-membered-ring hydrogen-bonding.
Macrocyclic compounds are an attractive class of therapeutic ligands against challenging targets, such as protein-protein interactions. However, the development macrocycles drugs is hindered by lack large combinatorial macrocyclic libraries, which cumbersome, expensive, and time consuming to make, screen, deconvolute. Here, we established a strategy for synthesizing screening libraries on picomolar scale using acoustic droplet ejection combine building blocks at nanoliter volumes, reduced...
Molecular self-assembly of nonamphiphilic α,β-hybrid foldamers based on urea-tethered anthranilic acid-proline (Ant-Pro) is reported. These self-assembled hollow vesicular architectures can take up and release the anticancer hydrophobic drug curcumin.
Structural modulation of Ant-Pro (anthranilic acid-proline) oligomers has been carried out by chirality alteration the proline residues. The results suggest that altered show well-defined helical conformation featuring nine-membered hydrogen bonding interactions - without compromising conformational rigidity.
Combination of three efficient chemical reactions allows for solution-phase synthesis 3780 macrocycles and identification potent thrombin inhibitor.
This communication describes the influence of β-aminobenzenesulfonic acid (<sup>S</sup>Ant) on conformational preferences hetero foldamers.
This communication describes a general synthetic route to bicyclic amino acid-carbohydrate-conjugates, which would be useful as conformationally restricted hydroxyethylamine (HEA) transition-state isosteres. The synthesis was achieved in 12 steps starting from D-glucose. striking features of this system are the rigid core displaying an α-amino acid side chain and moiety--both potentially important for receptor interactions, leading various biomedical responses, described literature. Crystal...
Abstract Macrocyclic compounds are an attractive class of therapeutic ligands against challenging targets, such as protein–protein interactions. However, the development macrocycles drugs is hindered by lack large combinatorial macrocyclic libraries, which cumbersome, expensive, and time consuming to make, screen, deconvolute. Here, we established a strategy for synthesizing screening libraries on picomolar scale using acoustic droplet ejection combine building blocks at nanoliter volumes,...