ReviewBioconjugate chemistry2009
Functionalized congener approach to the design of ligands for G protein-coupled receptors (GPCRs).
Review in Bioconjugate chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 47 citations in OpenAlex.
- Special issue of Medicinal Chemistry Research in honor of Dr. Kenneth A. Jacobson.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- E. B. Hershberg Award: Taming Inflammation by Tuning Purinergic Signaling.Accounts of chemical research · 2025Article
- Functionalized Congeners of 2Cells · 2024Article
- New paradigms in purinergic receptor ligand discovery.Neuropharmacology · 2023Review
- AInternational review of neurobiology · 2023Article
- Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors.Journal of medicinal chemistry · 2022Article
- Potent and selective ARSC medicinal chemistry · 2021Article
- Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization.Methods in cell biology · 2021Review
- Purinergic Signaling: Impact of GPCR Structures on Rational Drug Design.ChemMedChem · 2020Review
- Allosteric Antagonism of the ACells · 2020Article
- Conjugable AEuropean journal of medicinal chemistry · 2020Article
- Fast, Efficient, and Versatile Synthesis of 6-amino-5-carboxamidouracils as Precursors for 8-Substituted Xanthines.Frontiers in chemistry · 2019Article
- Breakthrough in GPCR Crystallography and Its Impact on Computer-Aided Drug Design.Methods in molecular biology (Clifton, N.J.) · 2018Article
- Discovery of the First Environment-Sensitive Fluorescent Probe for GPR120 (FFA4) Imaging.ACS medicinal chemistry letters · 2017Article
- Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.ACS medicinal chemistry letters · 2015Article
- 4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.Journal of medicinal chemistry · 2014Article
- The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs.British journal of pharmacology · 2014Review
- 4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2YMedChemComm · 2013Article
- Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.Journal of medicinal chemistry · 2013Review
- Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.Biochemical pharmacology · 2013Article
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Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
Functionalized congeners, in which a chemically functionalized chain is incorporated at an insensitive site on a pharmacophore, have been designed from the agonist and antagonist ligands of various G protein-coupled receptors (GPCRs). These chain extensions enable a conjugation strategy for detecting and characterizing GPCR structure and function and pharmacological modulation. The focus in many studies of functionalized congeners has been on two families of GPCRs: those responding to extracellular purines and pyrimidines-i.e., adenosine receptors (ARs) and P2Y nucleotide receptors. Functionalized congeners of small molecule as ligands for other GPCRs and non-G protein coupled receptors have also been designed. For example, among biogenic amine neurotransmitter receptors, muscarinic acetylcholine receptor antagonists and adrenergic receptor ligands have been studied with a functionalized congener approach. Adenosine A(1), A(2A), and A(3) receptor functionalized congeners have yielded macromolecular conjugates, irreversibly binding AR ligands for receptor inactivation and cross-linking, radioactive probes that use prosthetic groups, immobilized ligands for affinity chromatography, and dual-acting ligands that function as binary drugs. Poly(amidoamine) dendrimers have served as nanocarriers for covalently conjugated AR functionalized congeners. Rational methods of ligand design derived from molecular modeling and templates have been included in these studies. Thus, the design of novel ligands, both small molecules and macromolecular conjugates, for studying the chemical and biological properties of GPCRs have been developed with this approach, has provided researchers with a strategy that is more versatile than the classical medicinal chemical approaches.
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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.