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高升华 副研究员

AA证件照

一、基本情况

高升华,男,山东临沂人,博士,副研究员。主要从事结构生物学导向的精准药物设计及广谱抗病毒药物的发现(冠状病毒、HIV、腺病毒、登革热及尼帕病毒等);主持国家自然科学基金、中国博士后基金、山东省和广东省自然科学基金4项课题;参与国家重点研发计划、国家自然科学基金面上项目、山东省重大基础研究计划等多项课题。近5年以(共)第一或通讯作者在J Med ChemActa Pharm Sin BEur J Med ChemExpert Opin Ther PatJ Org ChemOrg Process Res Dev等国际著名学术期刊发表SCI文章15篇;参编专著1部;申请国家发明专利9件,授权3件;获全国创新创业优秀博士后及第十五届全国医药卫生青年科技学术会议二等奖等。

通讯地址: 山东省济南市文化西路44号乐宝体育中国官方网站药物化学研究所

TEL: 13156191828;QQ: 1152574113

E-mail:shh_gao@163.com

二、研究领域

1、运用靶标结构生物学导向的精准药物设计及表型筛选进行先导化合物的发现与优化;

2、广谱抗耐药性抗病毒药物的发现(冠状病毒、HIV、腺病毒、登革热及尼帕病毒等);

3、药物合成工艺研究,包括工艺路线优化及新路线设计、手性药物合成与拆分等。

三、学习及工作经历

2023/12 至今,副研究员,乐宝体育中国官方网站

2020/08 - 2023/12,博士后,乐宝体育中国官方网站,合作导师:刘新泳

2017/09 - 2020/06,中国医药工业研究总院,药物化学,博士,导师:张福利

2014/09 - 2017/06,沈阳药科大学,应用化学(药化方向),硕士,导师:赵春杰

2010/09 - 2014/06;青岛大学,应用化学,学士

四、承担课题

1、国家自然科学基金青年基金,22307067,2024-01-01至2026-12-31,主持

2、山东省科学自然科学基金青年基金,ZR2022QH036,2023-01至2025-12,主持

3、中国博士后科学基金面上资助项目,2021M702003,2021-10至2023-10,主持

4、广东省基础与应用基础研究基金区域联合基金,2021A1515110740,2021-10至2024-10,主持

五、近五年代表性论文(限10篇)

1.Gao, S., Song, L., Sylvester, K., Mercorelli, B., Loregian, A., Toth, K., Weiße, R. H., Useini, A., Sträter, N., Yang, M., Ye, B., Tollefson, A. E.*, Müller, C. E.*, Liu, X.*, Zhan, P*. Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability.Journal of Medicinal Chemistry, 2023, 66, 23, 16426–16440

2.Gao, S., Sylvester, K., Song, L., Claff, T., Jing, L., Woodson, M., Weiße, R. H., Cheng, Y., Schäkel, L., Petry, M., Gütschow, M., Schiedel, A. C., Sträter, N., Kang, D., Xu, S., Toth, K., Tavis, J., Tollefson, A. E.*, Müller, C. E.*, Liu, X.*, Zhan, P.*Discovery and Crystallographic Studies of TrisubstitutedPiperazine Derivatives as Non-Covalent SARS-CoV-2Main Protease Inhibitors with High TargetSpecificity and Low Toxicity.JournalofMedicinalChemistry, 2022, 65(19):13343-13364.(封面文章)

3.Gao, S.#, Song, L.#, Claff, T., Woodson, M., Sylvester, K., Jing, L., Weiße, R. H., Cheng, Y., Sträter, N., Schäkel, L., Gütschow, M., Ye, B., Yang, M., Zhang, T., Kang, D., Toth, K., Tavis, J., Tollefson, A. E.*, Müller, C. E.*, Zhan, P.*, Liu, X.*.Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivativesas Covalent SARS-CoV-2 Main Protease Inhibitors.JournalofMedicinalChemistry, 2022, 65(24):16902-16917.(封面文章)

4.Gao, S., Song, L., Cheng, Y., Zhao, F., Kang, D., Song, S., Yang, M., Ye, B., Zhao, W., Tang, Y., De Clercq, E., Pannecouque, C., Zhan, P.*, & Liu, X.*Discovery of Novel Sulfonamide Substituted Indolylarylsulfones as Potent HIV-1Inhibitorswith Better Safety Profiles.ActaPharmaceuticaSinicaB, 2023, 13(6):2747-2764.

5.Gao, S.#, Huang, T.#, Song, L., Xu, S., Cheng, Y., Cherukupalli, S., Kang, D., Zhao, T., Sun, L., Zhang, J., Zhan, P.*, Liu, X.* Medicinal chemistry strategies towards the development of effective SARS-CoV-2inhibitors.ActaPharmaceuticaSinicaB,2022, 12(2): 581-599.

6. Song, L.#,Gao, S.#, Ye, B., Yang, M., Cheng, Y., Kang, D., Yi, F., Sun, J. P., Menéndez-Arias, L., Neyts, J., Liu, X.*, Zhan, P.* Medicinal Chemistry Strategies Towards the Development of Non-covalent SARS-CoV-2 Mpro Inhibitors.ActaPharmaceuticaSinicaB,2024.14(1), 87–109

7.Gao, S.#, Cheng, Y.#, Song, S., Song, L., Zhao, F., Xu, S., Kang, D., Sun, L., Gao, P., De Clercq, E., Pannecouque, C., Liu, X.*, Zhan, P.*Chemicalspace exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1NNRTIs with spiro structural features.European Journal of Medicinal Chemistry, 2022, 238:114471.

8.Zhang, J.#, Dong, Y.#,Gao, S.#, Zhang, X., Liao, H., Shi, X., Zhang, Z., Zhao, T., Liang, R., Qi, D., Wu, T., Pang, J., Liu, X.*, Zhan, P.*Design, synthesis and activity evaluation of novel lesinurad analogues containing thienopyrimidinone or pyridine substructure as human urate transporter 1 inhibitors.European Journal of Medicinal Chemistry; 2022, 244:114816.

9.Gao, S.,Gao, X., Wu, Z., Li, H., Yang, Z., Zhang, F.*Process for (S)-Ketamine and (S)-Norketamine via Resolution Combined with Racemization.Journal of Organic Chemistry. 2020; 85(13): 8656-8664.

10.Gao, S., Gao, X., Yang, Z., Zhang, F.*, Process Research and Impurity Control Strategy of Esketamine;Organic Process Research & Development, 2020, 24(4), 555–566