1H-imidazo [4, 5-c] quinolin-4-amines: novel non-xanthine adenosine antagonists

…, I Van Wijngaarden, AP Ijzerman… - Journal of medicinal …, 1991 - ACS Publications
On the basis of a model we recently developed for the antagonist binding site of the adenosine
At receptor (J. Med. Chem. 1990, 33, 1708-1713), it was predicted that lH-imidazo [4, 5-c] …

N4-Unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands

…, MH van Amstel, MTM Tulp, AP IJzerman - Journal of medicinal …, 1995 - ACS Publications
In orderto explore the structural requirements for high 5-HTia affinity, a series of arylsubstituted
IW-phenylpiperazines were synthesized and evaluated for their ability to displace [3H]-8-…

The Concise Guide to PHARMACOLOGY 2021/22: G protein‐coupled receptors

…, L Hunyady, A Husain, AP IJzerman… - British journal of …, 2021 - Wiley Online Library
The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial
publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key …

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

…, V Cherezov, EYT Chien, JR Lane, AP IJzerman… - Science, 2008 - science.org
The adenosine class of heterotrimeric guanine nucleotide–binding protein (G protein)–coupled
receptors (GPCRs) mediates the important role of extracellular adenosine in many …

International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors

BB Fredholm, AP IJzerman, KA Jacobson… - Pharmacological …, 2001 - ASPET
Four adenosine receptors have been cloned and characterized from several mammalian
species. The receptors are named adenosine A 1 , A 2A , A 2B , and A 3 . The A 2A and A 2B …

Structural basis for allosteric regulation of GPCRs by sodium ions

…, GW Han, CB Roth, LH Heitman, AP IJzerman… - Science, 2012 - science.org
Pharmacological responses of G protein–coupled receptors (GPCRs) can be fine-tuned by
allosteric modulators. Structural studies of such effects have been limited due to the medium …

The Concise Guide to PHARMACOLOGY 2019/20: G protein‐coupled receptors

…, L Hunyady, A Husain, AP Ijzerman… - British journal of …, 2019 - Wiley Online Library
The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial
publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 …

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors—an update

BB Fredholm, AP IJzerman, KA Jacobson… - Pharmacological …, 2011 - ASPET
In the 10 years since our previous International Union of Basic and Clinical Pharmacology
report on the nomenclature and classification of adenosine receptors, no developments have …

[HTML][HTML] Beyond the hype: deep neural networks outperform established methods using a ChEMBL bioactivity benchmark set

…, HWT Van Vlijmen, W Kowalczyk, AP IJzerman… - Journal of …, 2017 - Springer
The increase of publicly available bioactivity data in recent years has fueled and catalyzed
research in chemogenomics, data mining, and modeling approaches. As a direct result, over …

Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists

…, VP Jaakola, JR Lane, J Lin, AP IJzerman… - Journal of medicinal …, 2010 - ACS Publications
The recent progress in crystallography of G-protein coupled receptors opens an unprecedented
venue for structure-based GPCR drug discovery. To test efficiency of the structure-based …