PhD candidate / guest
Xue Yang is a Ph.D. student at the Division of Drug Discovery & Safety. Her research works on covalent antagonists of G protein-coupled receptors, a case of adenosine receptors.
I studied medicinal chemistry at China Pharmaceutical University from September 2007 to June 2014 to obtain both my bachelor and master degree. In the last year of my bachelor study, I did one internship to perform the structure modification on the nature product, XJP, possessing anti-hypotension activity. During the three years of my master study, I designed and synthesized three series of the hydrogen sulfide-releasing compounds coupled with XJP, mainly isochroman-4 derivatives, and evaluated their vasodilating activities.
In September 2014, I was sponsored by China Scholarship Council to perform my PhD study at Leiden University under the supervision of Prof. Dr. A.P. IJzerman and Dr J.Louvel. My research works on covalent antagonists of G protein-coupled receptors, a case of adenosine receptors. In this case, I will design and synthesize compounds covalently binding to the adenosine receptors and evaluate their affinity, selectivity and degree of covalent binding. Aided by computer docking modeling and site-directed mutagenesis, more information will be clear on receptor binding site, possible binding motifs, protein functions and up-and down-regulation of receptor activity.
- Yang X., Dilweg M.A., Osemwengie D., Burggraaff L., Es D. van der, Heitman L.H. & IJzerman A.P. (2020), Design and pharmacological profile of a novel covalent partial agonist for the adenosine A1 receptor, Biochemical Pharmacology 180: 114144.
- Yang X. (4 December 2019), To bind or not to bind, that is an important question! : Development of covalent probes for adenosine receptors (PhD thesis. Leiden Academic Centre for Drugs Research (LACDR), Faculty of Science, Leiden University). Supervisor(s) and Co-supervisor(s): IJzerman A.P., Heitman L.H., Louvel J., Es D. van der.
- Yang X., Veldhoven J.P.D. van, Offringa J., Kuiper B.J., Lenselink E.B., Heitman L.H., Es D. van der & IJzerman A.P. (2019), Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor, Journal of Medicinal Chemistry 62(7): 3539-3552.
- Rouquette M., Lepetre-Mouelhi S., Dufrancais O., Yang X., Mougin J., Pieters G., Garcia-Argote S., IJzerman A.P. & Couvreur P. (2019), Squalene-Adenosine Nanoparticles: Ligands of Adenosine Receptors or Adenosine Prodrug?, Journal of Pharmacology and Experimental Therapeutics 369(1): 144-151.
- Yang X., Michiels T.J.M., Jong C. de, Soethoudt M., Dekker N., Gordon E., Stelt M. van der, Heitman L.H., Es D. van der & IJzerman A.P. (2018), An Affinity-Based Probe for the Human Adenosine A(2A) Receptor, Journal of Medicinal Chemistry 61(17): 7892-7901.
- Xia L., Vries H. de, Yang X., Lenselink E.B., Kyrizaki A., Barth F., Louvel J., Dreyer M.K., Es D. van der, IJzerman A.P. & Heitman L.H. (2018), Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism, Biochemical Pharmacology 151: 166-179.
- Yang X., Dong G., Michiels T.J.M., Lenselink E.B., Heitman L.H., Louvel J.A. & IJzerman A.P. (2017), A covalent antagonist for the human adenosine A_2A receptor, Purinergic signalling 13(2): 191-201.
No relevant ancillary activities