ArticleNature chemistry2011
A biomimetic polyketide-inspired approach to small-molecule ligand discovery.
Article in Nature chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed.
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- Re-Engineering of Yohimbine's Biological Activity through Ring Distortion: Identification and Structure-Activity Relationships of a New Class of Antiplasmodial Agents.ACS infectious diseases · 2020Article
- Chemical composition of DNA-encoded libraries, past present and future.Organic & biomolecular chemistry · 2019Review
- Solid-Phase Synthesis of β-Amino Ketones Via DNA-Compatible Organocatalytic Mannich Reactions.ACS combinatorial science · 2018Article
- One-Bead-Two-Compound Thioether Bridged Macrocyclic γ-AApeptide Screening Library against EphA2.Journal of medicinal chemistry · 2017Article
- Combinatorial chemistry in drug discovery.Current opinion in chemical biology · 2017Review
- Asymmetric synthesis of vinylogous β-amino acids and their incorporation into mixed backbone oligomers.Organic & biomolecular chemistry · 2017Article
- A Tryptoline Ring-Distortion Strategy Leads to Complex and Diverse Biologically Active Molecules from the Indole Alkaloid Yohimbine.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- High-throughput Identification of DNA-Encoded IgG Ligands that Distinguish Active and Latent Mycobacterium tuberculosis Infections.ACS chemical biology · 2017Article
- An unusual intramolecularTetrahedron · 2016Article
- Chemical Tools To Monitor and Manipulate Adaptive Immune Responses.Journal of the American Chemical Society · 2016Review
- Towards vast libraries of scaffold-diverse, conformationally constrained oligomers.Chemical communications (Cambridge, England) · 2016Article
- Peptidines: glycine-amidine-based oligomers for solution- and solid-phase synthesis.Chemical science · 2016Article
- Targeting Stereotyped B Cell Receptors from Chronic Lymphocytic Leukemia Patients with Synthetic Antigen Surrogates.The Journal of biological chemistry · 2016Article
- High affinity binding of conformationally constrained synthetic oligomers to an antigen-specific antibody: Discovery of a diagnostically useful synthetic ligand for murine Type 1 diabetes autoantibodies.Bioorganic & medicinal chemistry letters · 2015Article
- DNA-Encoded Solid-Phase Synthesis: Encoding Language Design and Complex Oligomer Library Synthesis.ACS combinatorial science · 2015Article
- Clustered distribution of natural product leads of drugs in the chemical space as influenced by the privileged target-sites.Scientific reports · 2015Article
- Direct comparison of linear and macrocyclic compound libraries as a source of protein ligands.ACS combinatorial science · 2015Article
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6 authors.
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Abstract
The discovery of new compounds for the pharmacological manipulation of protein function often embraces the screening of compound collections, and it is widely recognized that natural products offer beneficial characteristics as protein ligands. Much effort has therefore been focused on 'natural product-like' libraries, yet the synthesis and screening of such libraries is often limited by one or more of the following: modest library sizes and structural diversity, conformational heterogeneity and the costs associated with the substantial infrastructure of modern high-throughput screening centres. Here, we describe the design and execution of an approach to this broad problem by merging principles associated with biologically inspired oligomerization and the structure of polyketide-derived natural products. A novel class of chiral and conformationally constrained oligomers is described (termed 'chiral oligomers of pentenoic amides', COPA), which offers compatibility with split-and-pool methods and can be screened en masse in a batch mode. We demonstrate that a COPA library containing 160,000 compounds is a useful source of novel protein ligands by identifying a non-covalent synthetic ligand to the DNA-binding domain of the p53 transcription factor.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.