308 search results for “g protein-coupled receptor” in the Public website

• Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors Research output

  The present thesis focuses on the pharmacological concept of drug-target interaction, which dates back to the beginning of modern pharmacology.

• Better ligands for G Protein-Coupled Receptors Research project

  The receptor nomenclature committee of IUPHAR, the International Union of Pharmacology, has several subgroups. Among these are a few that our division is involved in, those for adenosine, nicotinic acid, and GnRH receptors.

• Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors Research project

  Supervisor: Xue Yang

• The activation mechanisms of G protein-coupled receptors: the case of the adenosine A2B and HCA2/3 receptors Research output

  Promotor: A.P. IJzerman

• Allosteric modulation by sodium ions and amilorides of G protein-coupled receptors Research output

  Promotor: A.P. IJzerman

• space smarter: Artificial intelligence in drug design for G protein-coupled receptors Research output

  Over several decades, a variety of computational methods for drug discovery have been proposed and applied in practice. With the accumulation of data and the development of machine learning methods, computational drug design methods have gradually shifted to a new paradigm, i.e. deep learning methods…

• decipher the interaction between the adenosine A2B receptor and the C-terminus of different G protein α-subunits. Research output

  Source: Purinergic Signal., Volume 10, Issue 3, pp. 441-53 (2014)

• the NPxxY(x)(5,6)F motif and helix 8 of the adenosine A(2B) receptor in G protein coupling Research output

  Source: Biochem Pharmacol, Volume 95, Issue 4, pp. 290-300 (2015)

• Novel receptor concepts Research project

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• to insurmountability: Novel avenues to better target CC Chemokine receptors Research output

  This thesis explores different avenues to develop insurmountable antagonists for CC Chemokine Receptors, such as CCR1, CCR2 and CCR5.

• Receptor Residence Time Research project

  Research question

• Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands Research project

  Supervisor: Andrea Martella

• 
  Adriaan IJzerman Professor emeritus Pharmacochemistry

  Science

• The ins and outs of ligand binding to CCR2 Research output

  Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: Dr. L.H. Heitman

• 
  Laura Heitman Professor Molecular Pharmacology

  Science

• Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines Research output

  Source: Biosens Bioelectron, Volume 74, pp. 233-42 (2015)

• investigating kinetic interactions between drug, endogenous neuropeptides and receptor Research output

  Promotor: A.P. IJzerman Co-promotor: L.H. Heitman

• Sodium ion binding pocket mutations and adenosine A2A receptor function Research output

  Source: Mol Pharmacol, Volume 87, Issue 2, pp. 305-13 (2015)

• Synthetic carbohydrate ligands for immune receptors Research output

  One of the main challenges in the development of an effective anti-cancer vaccine is the generation of an adequate and directed cellular immune response.

• Clavis Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands Research output

  Promotores: A.P. IJzerman, H.W.T. van Vlijmen

• Biophysical characterization of membrane protein-small molecule interactions Research output

  Promotor: M. Ubbink, Co-promotor: G. Siegal

• Allosteric modulation by sodium ions and amilorides of G protein- coupled receptors Research output

  Promotor: A.P. IJzerman

• Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors Research output

  The indane (2,3-dihydro-1H-indene) ring system is an attractive scaffold for biologically active compounds due to the combination of aromatic and aliphatic properties fused together in one rigid system.

• A chemical biology approach for targeting of ligand-drug conjugates Research output

  Promotores: Prof.dr. H. S. Overkleeft, Prof.dr. G. A. van der Marel

• Chemical tools to study the cannabinoid receptor type 2 Research output

  The cannabinoid receptor type 2 (CB2R) is associated with several inflammatory diseases with an unmet medical need (e.g. Alzheimers, multiple sclerosis, reumatoid arthritis). Development of new chemical biology strategies to study this protein is essential to aid future development of drugs for these…

• Physiological significance of the glucocorticoid and mineralocorticoid receptor signaling in the innate immune system Research project

  Does the mineralocorticoid receptor play a role in the effects of cortisol and synthetic glucocorticoids on the immune response?

• Liver X receptor: therapeutic targeting of common pathways in Psoriasis and Cardiovascular co-morbidities Research project

  Both psoriasis and atheroslcerosis are diseases characterized by a chronic and systemic inflammatory profile with local lipid disturbances that alter the barrier function of the skin (psoriasis) and cause the development of atherosclerotic plaques (atherosclerosis).

• Quantitative live cell imaging of glucocorticoid receptor dynamics in the nucleus Research output

  In this thesis, the focus lies on studying glucocorticoid receptor dynamics in living cells with the aim of understanding how this transcription factor finds its DNA target sites to regulate transcription.

• More effective blocking of CCR2 receptor Leiden Early Drug Discovery & Development

  The discovery of new medicines is a tedious and lengthy process. On average, over 10,000 molecules need to be studied for one to become a drug and reach the patient. Part of that process are the very costly clinical trials in humans, and candidate drugs often fail due to side effects or lack of efficacy.…

• Drug-target residence time: a case for the adenosine A1 and A2A receptors Research output

  Promotor: Prof.dr. A.P. IJzerman, Co-Promotor: Dr. L.H. Heitman

• action : target binding kinetics and functional efficacy at the mGlu2 receptor Research output

  During the course of drug discovery translational steps are made.

• The Role of Target Binding Kinetics in Drug Discovery Research output

  Source: ChemMedChem (2015)

• Intracellular allosteric modulators for human CC chemokine receptors Research project

  Supervisor: Natalia Ortiz Zacarías

• The activation mechanisms of G protein-coupled receptors Event - 8 December 2016

  PhD Defence

• Proteins in harmony: Tuning selectivity in early drug discovery Research output

  This thesis describes the importance of being able to control the selectivity of potential drug candidates.

• When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as Research output

  Source: Eur J Med Chem (2015)

• Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors Event - 30 May 2018

  PhD Defence

• Kinetic profiling of positive allosteric modulators of the mGlu2 receptor Research project

  Supervisor: Maarten Doornbos

• Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists Research output

  Source: Eur J Med Chem, Volume 101, pp. 681-91 (2015)

• Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists Research output

  Structure-affinity relationship (SAR) and structure-kinetics relationship (SKR) studies were combined to investigate a series of biphenyl anthranilic acid agonists for the HCA2 receptor.

• biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2) Research output

  Source: Bioorg Med Chem, Volume 23, Issue 14, pp. 4034-49 (2015)

• Kinetics for Drug Discovery: a Case for the Adenosine A3 receptor Research project

  Supervisor: Lizi Xia

• 
  G Dijkman

  Faculteit Geneeskunde

• 
  G Jukema

  Faculteit Geneeskunde

• 
  G Kleiverda

  Faculteit Geneeskunde

• 
  G Tavilla

  Faculteit Geneeskunde

• Agonists for the Adenosine A1 Receptor with Tunable Residence Time. A Case for Nonribose 4-Amino-6-aryl-5-cyano-2-thiopyrimidines Research output

  Source: J Med Chem, Volume 57, Issue 8, pp. 3213-22 (2014)

• 
  G van Drunen

  Faculteit Geneeskunde

• 
  G Trimbos-Kemper

  Faculteit Geneeskunde

• As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor Research output

  Animal models suggest that the chemokine ligand 2/CC-chemokine receptor 2 (CCL2/CCR2) axis plays an important role in the development of inflammatory diseases. However, CCR2 antagonists have failed in clinical trials because of a lack of efficacy.