Design, Synthesis, and Evaluation of New P2Y2 Receptor Antagonists and Fluorescent Ligands

QR Code

Design, Synthesis, and Evaluation of New P2Y2 Receptor Antagonists and Fluorescent Ligands

The P2Y2 receptor (P2Y2R) is an exciting therapeutic target for numerous diseases including atherosclerosis, idiopathic pulmonary fibrosis, and cancer. Despite this, there are a limited number of receptor antagonists available, none of which are clinically viable. The highest affinity P2Y2R antagoni...

Full description

Bibliographic Details
Main Author:	Knight, Rebecca
Format:	Thesis (University of Nottingham only)
Language:	English
Published:	2025
Subjects:	antagonists fluorescent ligands P2Y2R receptor antagonists drug development
Online Access:	https://eprints.nottingham.ac.uk/80213/

Similar Items

Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925
by: Conroy, Sean, et al.
Published: (2018)

From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor
by: Kindon, Nicholas, et al.
Published: (2017)

Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma
by: Sandham, David A., et al.
Published: (2017)

Illuminating the life of the adenosine receptors: development and application of subtype-selective fluorescent probes for the study of the human A1 and A2A adenosine receptors in living cells
by: Comeo, Eleonora
Published: (2022)

Cubyl amides: Novel P2X7 receptor antagonists
by: Gunosewoyo, Hendra, et al.
Published: (2008)

Purinergic P2X7 Receptor Antagonists: Chemistry and Fundamentals of Biological Screening
by: Gunosewoyo, Hendra, et al.
Published: (2009)

The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA3 adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition
by: Cheong, S., et al.
Published: (2010)

Optimisation of Peptide Linker-based Fluorescent Ligands for the Histamine H1 Receptor
by: Kok, Zhi Yuan
Published: (2020)

Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15
by: Liu, Mengjie, et al.
Published: (2016)

Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists
by: Kindon, Nicholas, et al.
Published: (2017)

Design, synthesis and pharmacological evaluation of novel fluorescent ligands for the mu-opioid receptor
by: Marshall, William
Published: (2021)

Investigating ligand-directed signalling at the cannabinoid receptor 2
by: Hourani, Wafa
Published: (2019)

Design and evaluation of fluorescent and non-fluorescent bivalent ligands to explore their mode of action at neuropeptide Y receptors
by: Richardson, Rachel
Published: (2019)

Fluorescent cannabinoids: Stratagies towards the synthesis of fluorescently labelled CB2 receptor ligands
by: Yates, Andrew Stephen
Published: (2005)

UDP-sugars activate P2Y 14 receptors to mediate vasoconstriction of the porcine coronary artery
by: Abbas, Zainab S.B., et al.
Published: (2018)

The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors
by: Kilpatrick, Laura E., et al.
Published: (2016)

Small molecule-based fluorescent probes as tool compounds for chemokine receptors CXCR4 and ACKR3
by: Dekkers, Sebastian
Published: (2019)

Characterization of Pectobacterium carotovorum and P. wasabiae and their potential control using antagonistic bacteria
by: Golkhandan, Elham
Published: (2014)

Imaging Cannabinoid Receptors: A Brief Collection of Covalent and Fluorescent Probes for CB1 and CB2 Receptors
by: Hamilton, A.J., et al.
Published: (2021)

Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors
by: Kilpatrick, Laura E., et al.
Published: (2012)

Potential Of Selected Antagonistic Bacteria In Controlling Damping-Off Disease Of Brassica Chinensis L. Caused By Pythium Myriotylum Drech
by: Zahara, Hafni
Published: (2004)

Molecular Probes for P2X7 Receptor Studies
by: Gunosewoyo, Hendra, et al.
Published: (2007)

Identification and characterisation of the P2Y14 purine receptor in the porcine coronary artery
by: Abbas, Z.S.B
Published: (2017)

Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism
by: Corriden, Ross, et al.
Published: (2014)

The design, synthesis and characterisation of subtype selective dipeptide-linked fluorescent ligands for human β1 and β2–adrenoceptors
by: Santu, L.T.
Published: (2017)

Agonist stimulus trafficking by human prostanoid CRTH2 (DP2) receptors.
by: McArthur Wilson, Richard John
Published: (2007)

Real-time analysis of the binding of fluorescent VEGF₁₆₅a to VEGFR2 in living cells: Effect of receptor tyrosine kinase inhibitors and fate of internalized agonist-receptor complexes
by: Kilpatrick, Laura E., et al.
Published: (2017)

Novel vasocontractile role of the P2Y14receptor: characterization of its signalling in porcine isolated pancreatic arteries
by: Alsaqati, M., et al.
Published: (2014)

Measuring ligand concentration where it matters: Assessing the “micro pharmacokinetic/pharmacodynamics” of adenosine receptor ligands
by: Lochray, Jack
Published: (2022)

Effect of memantine on rat and human NMDA receptors in comparison with harmonia axyridis extract
by: Rehman, Abdul
Published: (2023)

Synthesis and biological evaluation of novel PqsR antagonists to combat Pseudomonas aeruginosa infections
by: Mashabi, Alaa
Published: (2021)

Real-time ligand binding of fluorescent VEGF-A isoforms that discriminate between VEGFR2 and NRP1 in living cells
by: Peach, Chloe J., et al.
Published: (2018)

Active search for computer-aided drug design
by: Oglic, Dino, et al.
Published: (2018)

Chemical and in silico exploration of novel 5-hydroxytryptamine 2A receptor (5-HT2AR) ligands
by: Damerum, Luke
Published: (2024)

Potential use of selected antagonistic bacteria to control foot rot disease of black pepper (Piper nigrum L.) in Sarawak, Malaysia
by: Md Daut, Siti Noor Farhana
Published: (2014)

PAMFix, a fixative developed to enable remote platelet function testing: uses and applications
by: Heptinstall, Stan, et al.
Published: (2015)

P2X purinergic receptor ligands: recently patented compounds
by: Gunosewoyo, Hendra, et al.
Published: (2010)

Structural investigation of Pseudomonas aeruginosa quorum sensing receptor PqsR to aid virulence inhibition
by: Richardson, William
Published: (2022)

Endocrine and immune responses to resistance training in prostate cancer patients
by: Galvao, D, et al.
Published: (2008)

Biological significance of human epidermal growth factor receptor 2 (HER2) in breast cancer: effect of oestrogen receptor
by: Ahmad, Dena Akram Jerjees
Published: (2016)