User profiles for Lauren T. May
 | Lauren Therese MayMonash University Verified email at monash.edu Cited by 4669 |
Allosteric modulation of G protein–coupled receptors
The past decade has witnessed a significant growth in the identification of allosteric modulators
of G protein–coupled receptors (GPCRs), ie, ligands that interact with binding sites that …
of G protein–coupled receptors (GPCRs), ie, ligands that interact with binding sites that …
A kinetic view of GPCR allostery and biased agonism
… A receptor may adopt different conformations as it engages different … stars) may have different
residence times (t x or t y ) on the receptor. The duration of a ligand–receptor complex may …
residence times (t x or t y ) on the receptor. The duration of a ligand–receptor complex may …
Insights into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; advantages and pitfalls of differing methodologies
It is clear that the G protein‐coupled receptor family play a key role in the pharmaceutical
industry, with a significant proportion of approved drugs targeting this protein class. While our …
industry, with a significant proportion of approved drugs targeting this protein class. While our …
Structure of the adenosine-bound human adenosine A1 receptor–Gi complex
The class A adenosine A 1 receptor (A 1 R) is a G-protein-coupled receptor that preferentially
couples to inhibitory G i/o heterotrimeric G proteins, has been implicated in numerous …
couples to inhibitory G i/o heterotrimeric G proteins, has been implicated in numerous …
[PDF][PDF] Structure of the adenosine A1 receptor reveals the basis for subtype selectivity
The adenosine A 1 receptor (A 1 -AR) is a G-protein-coupled receptor that plays a vital role
in cardiac, renal, and neuronal processes but remains poorly targeted by current drugs. We …
in cardiac, renal, and neuronal processes but remains poorly targeted by current drugs. We …
Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia
… may elicit dose-limiting side effects such as bradycardia 9 . Limitations of orthosteric A 1 R
activators may … Recent advances in structural biology may help to identify allosteric sites within …
activators may … Recent advances in structural biology may help to identify allosteric sites within …
[HTML][HTML] Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
… Here we demonstrate that FPR1/FPR2-biased agonism may represent a novel therapeutic
strategy for the treatment of MI. The small-molecule FPR1/FPR2 agonist, Compound 17b (…
strategy for the treatment of MI. The small-molecule FPR1/FPR2 agonist, Compound 17b (…
Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist
The concepts of allosteric modulation and biased agonism are revolutionizing modern
approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). …
approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). …
Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands
Background and purpose: The introduction of fluorescence‐based techniques, and in
particular the development of fluorescent ligands, has allowed the study of G protein‐coupled …
particular the development of fluorescent ligands, has allowed the study of G protein‐coupled …
Dominant negative G proteins enhance formation and purification of agonist-GPCR-G protein complexes for structure determination
…, A Glukhova, TT Truong, LT May… - ACS pharmacology & …, 2018 - ACS Publications
Advances in structural biology have yielded exponential growth in G protein-coupled receptor
(GPCR) structure solution. Nonetheless, the instability of fully active GPCR complexes with …
(GPCR) structure solution. Nonetheless, the instability of fully active GPCR complexes with …