YU Haibo
Principal Investigator
Dr. Yu received her Ph.D. degree in the Department of Pharmacology of Peking Union Medical College in 2005. She finished her postdoctoral training in the Department of Neuroscience and Ion Channel Center, Johns Hopkins University School of Medicine from 2008 to 2013. She joined the Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College and was appointed as a Principal Investigator in March of 2014. Dr. Yu has been working on high-throughput drug screening targeting ion channels with a lot of experience since 2008. She is mainly interested in disease-related ion channels, establishing an ion channel drug research and development platform, discovering novel ion channel drugs and conducting research on small molecule regulation mechanism for nervous excitability diseases. She has published more than 20 papers in high-profile scientific journals.
1. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1.3 potassium channel blocker.Bri J Pharmacol . 2021, 178(13):2617-2631.
2. 4,5 caffeoylquinic acid and scutellarin, identified by integrated metabolomics and proteomics approach as the active ingredients of Dengzhan Shengmai, act against chronic cerebral hypoperfusion by regulating glutamatergic and GABAergic synapses. Pharmacological Research. 2020, 152, 104636. SCI 5.893.
3. Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABAA1 receptor with potent anticonvulsant activity and low toxicity. Europe Journal of Medicinal Chemistry. 2020, 185:111824. SCI 5.573.
4. Three new phenylspirodrimane derivatives with inhibitory effect towards potassium channel Kv1.3 from the fungus Stachybotrys chartarum. J Asian Nat Prod Res. 2019, 21(9):887-894.
5. Identification of WB4101, an alpha1-adrenoceptor antagonist, as a sodium channel blocker. Mol Pharmacol. 2018, 94(2):896-906.
6. Loperamide inhibits sodium channels to alleviate inflammatory hyperalgesia. Neuropharmacology. 2017, 117: 282-291.
7. High throughput screening technologies for ion channels. Acta Pharmacol Sin. 2016, 37(1):34-43.
8. Investigation of miscellaneous hERG inhibition in large diverse compound collection using automated patch-clamp assay. Acta Pharmacol Sin . 2016,37(1):111-23.
9. Effect of Tyrphostin AG879 on Kv4.2 and Kv4.3 potassium channels. Brit J Pharmacol . 2015, 172(13):3370-82.
10. Four basic residues critical for the ion selectivity and pore blocker sensitivity of TMEM16A calcium-activated chloride channels. Proc Natl Acad Sci U S A . 2015, 112(11):3547-52.
11. Global analysis reveals families of chemical motifs enriched for HERG inhibitors. PLoS One. 2015, 10(2):e0118324.
12. Dynamic Subunit Stoichiometry Confers a Progressive Continuum of Pharmacological Sensitivity by KCNQ Channels. Proc Natl Acad Sci U S A. 2013, 110,8732-8737.
13. PIP2 alters pharmacological selectivity for epilepsy-causing KCNQ channels. Proc Natl Acad Sci U S A. 2013, 110, 8726-8731, .
14. Modulation of hERG potassium channel gating normalizes action potential duration prolonged by dysfunctional KCNQ1 potassium channel. Proc Natl Acad Sci U S A. 2012,109, 11866-11871.
15. Discovery, Synthesis, and Structure Activity Relationship of a Series of N-Aryl- bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener. ACS chem neurosci. 2011, 2, 572-577.
16. Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor. J Med Chem. 2012, 55, 6975-6979.
17. Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1 -tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator. Bioorg Med Chem Lett. 2012, 22, 5936-5941.
18. hERGCentral: a large database to store, retrieve, and analyze compound-human Ether-a-go-go related gene channel interactions to facilitate cardiotoxicity assessment in drug development. Assay Drug Dev Technol. 2011, 9, 580-588.
19. Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133. ACS Chem Biol. 2011, 6, 845-856.
20. Profiling diverse compounds by flux- and electrophysiology-based primary screens for inhibition of human Ether-a-go-go related gene potassium channels. Assay Drug Dev Technol. 2010, 8, 743-754.
21. Role of potassium channels in Abeta(1-40)-activated apoptotic pathway in cultured cortical neurons. J Neurosci Res. 2006, 84, 1475-1484.
1. High throughput methods for ion channels. Handbook of Ion Channels. Yu, H., and Li, M. Edited by Jie Zheng and Matthew C. Trudeau. CRC Press , Pages 199-210. Print ISBN: 978-1-4665-5140-4.
2. Identification of a novel, small molecule activator of KCNQ1 channels. Probe Reports from the NIH Molecular Libraries Program. Yu, H., Lin, Z., Xu, K., Huang, X., Long, S., Wu, M., McManus, O. B., Engers, J. L., Mattmann, M. E., Engers, D. W., Le, U. M., Lindsley, C. W., *Hopkins, C. R., and *Li, M. PMID: 23762928 [PubMed] , 2012.
3. A small molecule activator of KCNQ2 and KCNQ4 channels. Probe Reports from the NIH Molecular Libraries Program. Yu, H., Wu, M., Long, S., *Hopkins, C. R., Engers, J. L., Townsend, S. D., Lindsley, C. W., McManus, O. B., and *Li, M. PMID: 23658954 [PubMed], 2011.
4. Identification of a novel, small molecule inhibitor of KCNQ2 channels. Probe Reports from the NIH Molecular Libraries Program. Yu, H., Xu, K., Zou, B., Wu, M., McManus, O. B., Engers, J. L., Cheung, Y. Y., Salovich, J. M., *Hopkins, C. R., Lindsley, C. W., and *Li, M. PMID: 23658963 [PubMed], 2011.
5. A potent and selective small molecule Kir2.1 inhibitor. Probe Reports from the NIH Molecular Libraries Program. Wu, M., Wang, H., Yu, H., Makhina, E., Xu, J., Dawson, E. S., Hopkins, C. R., *Lindsley, C. W., McManus, O. B., and *Li, M. PMID: 21433384 [PubMed], 2010.
