Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery
RA Bond, AP IJzerman - Trends in pharmacological sciences, 2006 - cell.com
The concept of constitutively active G-protein-coupled receptors is now firmly rooted in receptor
pharmacology. Many independent research groups have contributed to its acceptance …
pharmacology. Many independent research groups have contributed to its acceptance …
[HTML][HTML] Inverse agonism at G protein-coupled receptors:(patho) physiological relevance and implications for drug discovery
…, AP Kourounakis, AP IJzerman - British journal of …, 2000 - ncbi.nlm.nih.gov
The largest family of cell surface receptors involved in signal transduction, G protein coupled
receptors (GPCRs), are one of the major targets for current drugs as well as new drug …
receptors (GPCRs), are one of the major targets for current drugs as well as new drug …
The RESOLUTE consortium: unlocking SLC transporters for drug discovery
…, BJ Bongers, LH Heitman, AP IJzerman… - Nature reviews Drug …, 2020 - nature.com
The Innovative Medicines Initiative Consortium RESOLUTE has started to develop tools and
produce data sets to de-orphanize transporters in the solute carrier protein (SLC) …
produce data sets to de-orphanize transporters in the solute carrier protein (SLC) …
Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor.
…, C Krasel, AP Ijzerman… - Proceedings of the …, 1996 - National Acad Sciences
To investigate the molecular mechanism for stereospecific binding of agonists to beta 2-adrenergic
receptors we used receptor models to identify potential binding sites for the beta-OH-…
receptors we used receptor models to identify potential binding sites for the beta-OH-…
New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A2B Receptor with an Improved Selectivity Profile Compared to the Reference Agonist N …
…, J Brussee, AP IJzerman - Journal of medicinal …, 2004 - ACS Publications
The adenosine A 2B receptor is the least well characterized of the four known adenosine
receptor subtypes because of the absence of potent, selective agonists. Here, we present five …
receptor subtypes because of the absence of potent, selective agonists. Here, we present five …
[HTML][HTML] A binding site model and structure-activity relationships for the rat A3 adenosine receptor
…, N Melman, ME Olah, AP IJzerman… - Molecular …, 1994 - ncbi.nlm.nih.gov
A novel adenosine receptor, the A 3 receptor, has recently been cloned. We have systematically
investigated the hitherto largely unexplored structure-activity relationships (SARs) for …
investigated the hitherto largely unexplored structure-activity relationships (SARs) for …
The molecule evoluator. An interactive evolutionary algorithm for the design of drug-like molecules
We developed a software tool to design drug-like molecules, the “Molecule Evoluator”, which
we introduce and describe here. An atom-based evolutionary approach was used allowing …
we introduce and describe here. An atom-based evolutionary approach was used allowing …
The adhesion G protein-coupled receptor G2 (ADGRG2/GPR64) constitutively activates SRE and NFκB and is involved in cell adhesion and migration
…, B Boogaard, KL Egerod, B van de Water, AP Ijzerman… - Cellular signalling, 2015 - Elsevier
Adhesion G protein-coupled receptors (ADGRs) are believed to be activated by auto-proteolytic
cleavage of their very large extracellular N-terminal domains normally acting as a …
cleavage of their very large extracellular N-terminal domains normally acting as a …
Evolutionary algorithms in drug design
Designing a drug is the process of finding or creating a molecule which has a specific activity
on a biological organism. Drug design is difficult since there are only few molecules that …
on a biological organism. Drug design is difficult since there are only few molecules that …
How to catch a membrane protein in action: a review of functional membrane protein immobilization strategies and their applications
V Fruh, AP IJzerman, G Siegal - Chemical reviews, 2011 - ACS Publications
Analysis of the results from the human proteome project suggests> 30% of proteins are
membrane bound. 1 Membrane proteins (MPs) are in the core group responsible for signal …
membrane bound. 1 Membrane proteins (MPs) are in the core group responsible for signal …