The exploration of macrocycles for drug discovery--an underexploited structural class.
about
Selected synthetic strategies to cyclophanesThe click reaction as an efficient tool for the construction of macrocyclic structuresGetting in shape: controlling peptide bioactivity and bioavailability using conformational constraintsInduced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease targetThe mechanism of patellamide macrocyclization revealed by the characterization of the PatG macrocyclase domainStructure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic propertiesThe discovery of new cyanobactins from Cyanothece PCC 7425 defines a new signature for processing of patellamidesImproving binding affinity and stability of peptide ligands by substituting glycines with D-amino acidsStructural and Thermodynamic Effects of Macrocyclization in HCV NS3/4A Inhibitor MK-5172Structural and Biochemical Basis for Intracellular Kinase Inhibition by Src-specific Peptidic MacrocyclesSynthesis of macrocyclic organo-peptide hybrids from ribosomal polypeptide precursors via CuAAC-/hydrazide-mediated cyclizationThe Melanocortin Receptor System: A Target for Multiple Degenerative DiseasesOxidative diversification of amino acids and peptides by small-molecule iron catalysisSynthesis of Hybrid Cyclopeptides through Enzymatic MacrocyclizationEnzymatic Macrocyclization of 1,2,3-Triazole Peptide MimeticsQ28828613Constraining cyclic peptides to mimic protein structure motifs.Ternatin and improved synthetic variants kill cancer cells by targeting the elongation factor-1A ternary complex.Ring-Expansion Approach to Medium-Sized Lactams and Analysis of Their Medicinal Lead-Like Properties.Translation of DNA into a library of 13,000 synthetic small-molecule macrocycles suitable for in vitro selection.Rapid selection of cyclic peptides that reduce alpha-synuclein toxicity in yeast and animal modelsExpanding the range of 'druggable' targets with natural product-based libraries: an academic perspective.In vitro selection of a DNA-templated small-molecule library reveals a class of macrocyclic kinase inhibitorsAn aldol-based build/couple/pair strategy for the synthesis of medium- and large-sized rings: discovery of macrocyclic histone deacetylase inhibitors.Cyanobacterial cyclopeptides as lead compounds to novel targeted cancer drugsEarly endosomal escape of a cyclic cell-penetrating peptide allows effective cytosolic cargo delivery.Large ring-forming alkylations provide facile access to composite macrocyclesDiversity-oriented synthesis of macrocyclic peptidomimetics.Fragment-based domain shuffling approach for the synthesis of pyran-based macrocycles.Fragmentation of bicyclic γ-silyloxy-β-hydroxy-α-diazolactones as an approach to ynolidesCrossing borders to bind proteins--a new concept in protein recognition based on the conjugation of small organic molecules or short peptides to polypeptides from a designed setHSP90 inhibitor, celastrol, arrests human monocytic leukemia cell U937 at G0/G1 in thiol-containing agents reversible wayRole of natural product diversity in chemical biology.Recent trends and observations in the design of high-quality screening collections.Metal-binding and redox properties of substituted linear and cyclic ATCUN motifs.On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds.Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.Development of a general, sequential, ring-closing metathesis/intramolecular cross-coupling reaction for the synthesis of polyunsaturated macrolactonesRedox-triggered self-assembly of gadolinium-based MRI probes for sensing reducing environmentBuild/couple/pair strategy for the synthesis of stereochemically diverse macrolactams via head-to-tail cyclization.
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P2860
The exploration of macrocycles for drug discovery--an underexploited structural class.
description
article científic
@ca
article scientifique
@fr
articolo scientifico
@it
artigo científico
@pt
bilimsel makale
@tr
scientific article published on July 2008
@en
vedecký článok
@sk
vetenskaplig artikel
@sv
videnskabelig artikel
@da
vědecký článek
@cs
name
The exploration of macrocycles for drug discovery--an underexploited structural class.
@en
The exploration of macrocycles for drug discovery--an underexploited structural class.
@nl
type
label
The exploration of macrocycles for drug discovery--an underexploited structural class.
@en
The exploration of macrocycles for drug discovery--an underexploited structural class.
@nl
prefLabel
The exploration of macrocycles for drug discovery--an underexploited structural class.
@en
The exploration of macrocycles for drug discovery--an underexploited structural class.
@nl
P2093
P356
P1476
The exploration of macrocycles for drug discovery--an underexploited structural class.
@en
P2093
Edward M Driggers
Nicholas K Terrett
Stephen P Hale
P2888
P304
P356
10.1038/NRD2590
P577
2008-07-01T00:00:00Z