Cited by 27Click Chemistry and ApplicationsChemical Synthesis and AnalysisBiochemical and Structural Characterization

Tailored Bioorthogonal and Bioconjugate Chemistry: A Source of Inspiration for Developing Kinetic Target-Guided Synthesis Strategies

Open access
Lossouarn, Alexis, Renard, Pierre-Yves, Sabot, Cyrille·2021·Bioconjugate Chemistry

Abstract

Kinetic target-guided synthesis (KTGS) is a promising tool for the discovery of biologically active compounds. It relies on the identification of potent ligands that are covalently assembled by the biological targets themselves from a pool of reagents. Significant effort is devoted to developing new KTGS strategies; however, only a handful of biocompatible reactions are available, which may be insufficient to meet the specificities (stability, dynamics, active site topology, etc.) of a wide range of biological targets with therapeutic potential. This Topical Review proposes a retrospective analysis of existing KTGS ligation tools, in terms of their kinetics and analogy with other biocompatible reactions, and provides new clues to expand the KTGS toolkit. By way of examples, a nonexhaustive selection of such chemical ligation tools belonging to different classes of reactions as promising candidate reactions for KTGS are suggested.

Integrity signals

Registry

Crossref · 10.1021/acs.bioconjchem.0c00568

Cites

93 of 93 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

We couldn’t retrieve this paper’s full text, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

  • Currently there are limited methods to selectively covalently bind to a protein.

    “Currently there are limited methods to selectively covalently bind to a protein56–58”

    From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [58]

Cites

Flagged first, then by citations

1 of the 94 references couldn’t be matched to a known paper.

Cited by

Sorted by citations

Authors
Lossouarn, A., Renard, P.-Y., & Sabot, C.
Affiliations
Centre National de la Recherche Scientifique (FR)
Corresponding author
Sabot, Cyrille
Venue
Bioconjugate Chemistry
Published
2020-11-24
Volume
32
Issue
1
Pages
63-72
ISSN
  • 1043-1802 (ISSN-L)
  • 1520-4812
OpenAlex
W3109296721
Cited by
26
References
94
Citations by year
2025: 3 · 2024: 11 · 2023: 5 · 2022: 4 · 2021: 3
FWCI
0.23
Type
journal article
Language
en
Locations
  • Bioconjugate Chemistry (publishedVersion)
  • PubMed (publishedVersion)
  • HAL (submittedVersion, other-oa)
Funders
  • Agence Nationale de la Recherche (ANR-11-LABX-0029, ANR-16-CE07-0004)
  • Universit? de Rouen
  • Centre National de la Recherche Scientifique
  • INSA Rouen Normandie
Topics
  • Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Structural Characterization
Keywords
bioorthogonal chemistry, bioconjugation, chemical ligation, covalent drug discovery, ligand discovery, reaction kinetics, active site topology
MeSH terms
Kinetics, Ligands, Retrospective Studies, Thermodynamics, Drug Discovery

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review