Results 31 to 40 of about 11,458 (225)

Chemical Synthesis and Functional Screening of an 800 000‐Member Library Using a Peptide‐Pairing Strategy

open access: yesAngewandte Chemie, EarlyView.
Chemical peptide synthesis allows the generation of structurally highly diverse compounds suited for ligand development, but current methods in parallel peptide synthesis limit the achievable library size to a few thousand. A strategy is presented based on combinatorial pairing of short peptides via disulfide linkage that enables the generation and ...
Anne Zarda   +5 more
wiley   +2 more sources

Well-Tempered MetaDynamics based method to evaluate universal peptidomimetics [PDF]

open access: yes, 2018
Peptidomimetics are a broad family of compounds designed to mimic the main structural features of peptides, avoiding their metabolic drawbacks. In particular, universal peptidomimetics use only peptide side-chain analogs to mimic different secondary ...
GANDINI, ENRICO   +4 more
core   +1 more source

Backbone Steric Constraints Underlie High Passive Membrane Permeability of N‐Alkyl Peptides

open access: yesAngewandte Chemie, EarlyView.
Beyond amide hydrogen removal, steric constraints encoded in N/Cα‐dually substituted backbones are uncovered as a key determinant of passive membrane permeability in N‐alkyl peptides. These constraints restrict conformational freedom and sterically limit backbone hydration during membrane permeation.
Ayumi Inayoshi   +8 more
wiley   +2 more sources

Downsizing the Histone H3–H4 Quaternary Structure Into Foldamer Mimetics Yields High‐Affinity and Cell‐Permeable Ligands of ASF1

open access: yesAngewandte Chemie, EarlyView.
We present a foldamer strategy to downsize the histone H3‐H4 quaternary structure into high‐affinity, medium‐sized binders (∼2 kDa) for the histone chaperone ASF1. Our peptide‐oligourea chimeras, designed through structure‐guided optimization and foldamer chemistry, recapitulate the natural H3‐H4 dimer binding mode while demonstrating plasma stability ...
Bo Li   +15 more
wiley   +2 more sources

Peptidomimetics : A New Era in Drug Discovery

open access: yesJournal of Pharmaceutical Research
Peptides are made up from amino acid sequences which possess importance in various biological processes, making them attractive candidates for therapeutic development.
Shubham N Karle   +2 more
doaj   +1 more source

Studies of Insulin Dicarba-Peptidomimetics

open access: yes, 2019
This thesis explores the chemical synthesis of novel insulin molecules. It identifies new synthetic strategies to afford molecules of this type, and evaluates the biological activity of the insulins synthesised.
ANDREW MAGNUS WRIGHT (6563372)
core   +1 more source

Beyond Simple Mimicry: Next‐Generation Geometric Architectures and Future Paradigms in Small‐Molecule and Macrocyclic Peptidomimetics

open access: yesAngewandte Chemie, EarlyView.
Peptide‐to‐Small Molecule Paradigm: Peptidomimetics have evolved from simple mimicry toward drug‐like scaffolds supported by increasing clinical successes. This Perspective highlights the geometric design principles—linear repetition, convergent fusion, and cyclization—defining the next‐generation peptidomimetic architectures capable of targeting ...
Jesang Lee   +5 more
wiley   +2 more sources

Short Cationic Peptidomimetic Antimicrobials

open access: yesAntibiotics, 2019
The rapid growth of antimicrobial resistance against several frontline antibiotics has encouraged scientists worldwide to develop new alternatives with unique mechanisms of action. Antimicrobial peptides (AMPs) have attracted considerable interest due to
Rajesh Kuppusamy   +3 more
doaj   +1 more source

Polyproline: A Synthetic Polypeptide With Unique Properties

open access: yesAngewandte Chemie, EarlyView.
Poly‐L‐proline is a unique polypeptide distinguished by its well‐defined secondary structures and unusual thermal behavior. This mini review highlights recent advances in the synthesis of poly‐L‐proline by N‐carboxyanhydride (NCA) polymerization, the formation of structurally defined architectures and nanostructures, and emerging strategies that ...
Rosanna Le Scouarnec   +3 more
wiley   +2 more sources

Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics

open access: yesBeilstein Journal of Organic Chemistry, 2014
In the recent past, the design and synthesis of peptide mimics (peptidomimetics) has received much attention. This because they have shown in many cases enhanced pharmacological properties over their natural peptide analogues.
Gijs Koopmanschap   +2 more
doaj   +1 more source

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