Helix mimetics small molecules
Web15 jun. 2024 · We synthesized small molecule mimetics of the α-helical domain of IRAK2 with drug-like characteristics based on the recent advances in the designing of α-helix … Web• Multistep synthesis of macrocycles and their metallo-complexes including N4O2-cyclic oxiimines, porphyrins, and pyrogallol [4]arenes • Design and synthesis of small and mid-sized molecules...
Helix mimetics small molecules
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WebSubstantial changes in function or immunological identity are made by selecting residues that differ more significantly in their effect on maintaining (a) the structure of the polypeptide backbone in the area of the substitution, for example as a sheet or helical conformation, (b) the charge or hydrophobicity of the molecule at the target site or (c) the bulk of the side … Web1 feb. 2014 · The rational design of helix mimetics is an appealing small-molecule strategy for the mediation of aberrant PPIs, however the first generation of scaffolds …
WebI am a peptide chemist, working as a Research Fellow at the University of Auckland in the area of peptides with antimicrobial activity. I recently completed my PhD at the University of Adelaide, which a specialising in peptides with defined secondary structure to investigate protein interactions. I am a driven early career researcher with excellent time … Web16 feb. 2024 · Furthermore, BTdCPU, a small-molecule activator of HRI, similarly triggers MCL-1 repression and synergizes with BH3-mimetics in mouse and human leukemia including both Ph+ and Ph-like B-ALL.
WebTamoxifen was the first ER-targeted small molecule to be approved for the treatment of women with ER + breast cancer. This molecule had initially been explored for use as an antiestrogenic contraceptive agent based on its activity in rodents but was found to stimulate rather than suppress ovulation in women, halting its progress within Imperial Chemical … WebSynthesis and screening of small-molecule α-helix mimetic libraries targeting protein-protein interactions. α-Helices are the most common protein secondary structure and …
Web11 feb. 2024 · Teraryl-based α-helix mimetics have proven to be useful compounds for the inhibition of protein-protein interactions (PPI). We have developed a modular and flexible … radisson youtubeWeb27 mrt. 2013 · Driven by the need to target these larger protein surfaces, there has been renewed interest in recent years in developing larger therapeutic molecules, such as peptides and their mimetics, which can in principle combine advantages of proteins (target specificity, structural stability) with advantages of small molecules (lower cost, oral … radisson xingguo hotel shanghaiWeb1 jan. 2016 · The oxopiperazine helix mimetics can be assembled from α-amino acids using standard solid-phase peptide synthesis methodology, enabling rapid diversification of the scaffold and discovery of ligands for protein targets. We have evaluated the biological potential of the oxopiperazine mimetics in cell-free, cell culture, and in vivo models. radisson zaffron resortWeb12 mei 2014 · Small molecules that mimic the structural arrangement of the key residues on these helices should afford competitive inhibitors of HIF1α/p300 complex formation ( 19, 22 ). We used a recently described strategy from our groups to mimic the interacting face of an α-helix on a small-molecule oxopiperazine scaffold ( 31 ). radisson zaffron resort 5*Web19 mrt. 2024 · Teraryl-based alpha-helix mimetics have resulted in efficient inhibitors of protein-protein interactions (PPIs). Extending the concept to even longer oligoarene systems would allow for the mimicking of even larger interaction sites. radisson-warwickWebDesign of small molecules to mimic the structural features of peptides using active ... In these designs it is important that the synthetic scaffolds position the side chains consistently with the helical and turn structures. Maintaining the backbone hydrogen bonding interactions is the major task for β-sheet mimetics. These strategies ... radisys addressWeb1 feb. 2015 · We highlight HTS methods for the identification of small-molecule α-helix mimetics. α-Helices are the most common protein secondary structure and play a key … radisson-warwick hotel