Publications

Completed List of Published Papers for Haitao (Mark) Ji, Ph.D.

https://www.ncbi.nlm.nih.gov/myncbi/1vk-j93Cwoe5o/bibliography/public/

 

ORCID: 0000-0001-5526-4503

Researcher ID: P-6441-2015

Independent Research (^*: corresponding author; ^†: authors had equal contribution)

Original Research Papers

  2022

• Kell, Shelby R; Wang, Zhen; Ji, Haitao.* Common structural features of hydrophobic α-helical hot spots: Insights for the design of novel α-helix mimetics. ACS. Med. Chem. Lett. 2022. Articles ASAP. DOI: 10.1021/acsmedchemlett.2c00296
• Kell, Shelby R.; Wang, Zhen; Ji, Haitao.* Fragment hopping protocol for the design of small-molecule protein–protein interaction inhibitors. Bioorg. Med. Chem. 2022, 69, 116879.
• Wang, Zhen;^† Zhang, Min;^† Thompson, Harriet M.; Ji, Haitao.* New ZW4864 derivatives as small-molecule inhibitors for the β-catenin/BCL9 protein–protein interaction. ACS Med. Chem. Lett. 2022, 13 (5), 865–870.
• Wang, Zhen; Ji, Haitao.* Characterization of hydrophilic α-helical hot spots on the protein-protein interaction interfaces for the design of α-helix mimetics. J. Chem. Info. Model. 2022, 62 (8), 1873–1890.

  2021

• Xiao, Tao;^† Sun, Luxin;^† Zhang, Min; Li, Zilu; Haura, Eric B.; Schonbrunn, Ernst;* Ji, Haitao.* Synthesis and structural characterization of a monocarboxylic inhibitor of GRB2 SH2 domain. Bioorg. Med. Chem. Lett. 2021, 51, 128354.
• Wang, Zhen;^† Zhang, Min;^† Quereda, Victor;^† Frydman, Sylvia M.; Ming, Qianqian; Luca, Vincent C.; Duckett, Derek R.;* Ji, Haitao.* Discovery of an orally bioavailable small-molecule inhibitor for the β-catenin/B-cell lymphoma 9 protein-protein-protein interaction. J. Med. Chem. 2021, 64 (16):12109–12131.
• Li, Zilu;^† Zhang, Min;^† Teuscher, Kevin B.; Ji, Haitao.* Discovery of 1-benzoyl 4-phenoxypiperidines as small-molecule inhibitors of the β‑catenin/B-cell lymphoma 9 protein−protein interaction. J. Med. Chem. 2021, 64 (15), 11195–11218.
• Tafreshi, Narges K.; Pandya, Darpan N.; Tichacek, Christopher J.; Budzevich, Mikalai M.; Wang, Zhen; Reff, Jordan N.; Engelman, Robert W.; Boulware, David C.; Chiappori, Alberto A.; Strosberg, Jonathan R.; Ji, Haitao; Wadas, Thaddeus J.; El-Haddad, Ghassan;* Morse, David L.* Pre-clinical evaluation of ²²⁵Ac-DOTATATE for treatment of lung neuroendocrine neoplasms. Eur. J. Nucl. Med. Mol. Imaging 2021, 48 (11), 3408–3421.
• Wang, Zhen;^† Zhang, Min;^† Luo, Wen; Zhang, Yongqiang; Ji, Haitao.* Discovery of 2-(3-(3-carbamoylpiperidin-1-yl)phenoxy)acetic acid derivatives as novel small-molecule inhibitors of the β-catenin/B-cell lymphoma 9 protein−protein interaction. J. Med. Chem. 2021, 64 (9), 5886–5904.

  2020

• Li, Qingliang; Karim, Rezaul M.; Cheng, Mo; Das, Mousumi; Chen, Lihong; Zhang, Chen; Lawrence, Harshani R.; Daughdrill, Gary W.; Schonbrunn, Ernst, Ji, Haitao, Chen, Jiandong.* Inhibition of p53 DNA binding by a small molecule protects mice from radiation toxicity. Oncogene 2020, 39 (29), 5187–5200.

  2019

• Wang, Zhen; Ji, Haitao.* Targeting the side-chain convergence of hydrophobic α-helical hot spots to design small-molecule mimetics: Key binding features for i, i + 3, and i + 7.  J. Med. Chem. 2019, 62 (21), 9906–9917.
• Sang, Peng;^† Zhang, Min;^† Shi, Yan;^† Li, Chunpu; Abdulkadir, Sami; Li, Qi; Ji,* Haitao;* Cai, Jianfeng.* Inhibition of β-catenin/B-cell lymphoma 9 protein–protein interaction using α-helix-mimicking sulfono-γ-AApeptide inhibitors. Proc. Natl. Acad. Sci. U.S.A. 2019, 116 (22), 10757–10762.
• Wang, Zhen;^† Zhang, Min;^† Wang, Jin; Ji, Haitao.* Optimization of peptidomimetics as selective inhibitors for the β-catenin/T-cell factor protein–protein interaction. J. Med. Chem. 2019, 62 (7), 3617–3635.

  2018

• Wu, Xiaowei; Ji, Haitao.* Ruthenium-catalyzed C-H allylation of alkenes with allyl alcohols via C-H bond activation in aqueous solution. J. Org. Chem. 2018, 83 (19), 12094–12102.
• Wu, Xiaowei; Ji, Haitao.* Rhodium(III)-catalyzed C-H allylation of indoles with allyl alcohols via β-hydroxide elimination. Org. Biomol. Chem. 2018, 16 (31), 5691-5698.
• Huang, Chenfei; Cao, Zhe, Ma, Jun; Shen, Yi; Bu, Yiwen; Khoshaba, Ramina; Shi, Guiyuan; Huang, Dan; Liao, Duan-Fang; Ji, Haitao; Jin, Junfei;* Cao, Deliang.* AKR1B10 activates diacylglycerol (DAG) second messenger in breast cancer cells. Mol. Carcinog. 2018, 57 (10), 1300–1310.
• Wu, Xiaowei; Ji, Haitao.* Rhodium-catalyzed [4 + 1] cyclization via C-H activation for the synthesis of divergent heterocycles bearing a quaternary carbon. J. Org. Chem. 2018, 83 (8), 4650–4656.
• Zhang, Min;^† Wang, Zhen;^† Zhang, Yongqiang; Guo, Wenxing; Ji, Haitao.* Structure-based optimization of small-molecule inhibitors for the β-catenin/B-cell lymphoma 9 protein–protein interaction. J. Med. Chem.  2018, 61 (7), 2989–3007.
• Wu, Xiaowei; Ji, Haitao.* Ruthenium(II)-catalyzed regio- and stereoselective C−H allylation of indoles with allyl alcohols. Org. Lett. 2018, 20 (8), 2224–2227.

  2017

• Teuscher, Kevin B.; Zhang, Min; Ji, Haitao.* A versatile method to determine the cellular bioavailability of small-molecule inhibitors.  J. Med. Chem.  2017, 60 (1), 157–169. This paper is featured as ACS Editors' Choice and recommended by F1000 faculty! F1000 Prime Recommended

  2016

• Wisniewski, John A.; Yin, Jinya; Teuscher, Kevin B.; Zhang, Min; Ji, Haitao.* Structure-based design of 1,4-dibenzoylpiperazines as β-catenin/B-cell lymphoma 9 protein–protein interaction inhibitors.  ACS Med. Chem. Lett.  2016, 7 (5), 508–513.
• Zhang, Yongqiang; Teuscher, Kevin B.; Ji, Haitao.* Direct α-heteroarylation of amides (α to nitrogen) and ethers through a benzaldehyde-mediated photoredox reaction.  Chem. Sci.  2016, 7 (3), 2111–2118.

  2015

• Hoggard, Logan R.; Zhang, Yongqiang; Zhang, Min; Panic, Vanja; Wisniewski, John A.; Ji, Haitao.* Rational Design of selective small-molecule inhibitors for β-catenin/B-cell lymphoma 9 protein–protein interactions.  J. Am. Chem. Soc.  2015, 137 (38), 12249–12260.
• Catrow, J. Leon; Zhang, Yongqiang; Zhang, Min; Ji, Haitao.* Discovery of selective small-molecule inhibitors for the β-catenin/T-cell factor protein–protein interaction through the optimization of the acyl hydrazone moiety.  J. Med. Chem.  2015, 58 (11), 4678–4692.
• Zhang, Min; Wisniewski, John A.; Ji, Haitao.* AlphaScreen selectivity assay for β-catenin/B-cell lymphoma 9 inhibitors.  Anal. Biochem.  2015, 469, 43–53.

  2014

• Drury, Paul P.; Davidson, Joanne O.; Mathai, Sam; van den Heuji, Lotte G.; Ji, Haitao; Bennet, Laura; Tan, Sidhartha; Silverman, Richard B.; Gunn, Alistair J.* nNOS inhibition during profound asphyxia reduces seizure burden and improves survival of striatal phenotypic neurons in preterm fetal sheep.  Neuropharmacology  2014, 83C, 62–70.
• Huang, Zheng; Zhang, Min; Burton, Shawn D.; Katsakhyan, Levon N.; Ji, Haitao.* Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt β-catenin/T-cell factor protein–protein interactions.  ACS Chem. Biol.  2014, 9 (1), 193–201.

  2013

• Zhang, Min; Catrow, J. Leon; Ji Haitao.* High-throughput selectivity assays for small-molecule inhibitors of β-catenin/T-cell factor protein-protein interactions.  ACS Med. Chem. Lett.  2013, 4 (2), 306–311.
• Yu, Binxun; Huang, Zheng; Zhang, Min; Dillard, Darren R.; Ji, Haitao.* Rational design of small-molecule inhibitors for β-catenin/T-cell factor protein-protein interactions by bioisostere replacement.  ACS Chem. Biol.  2013, 8 (3), 524–529. Recommended by the F1000 Faculty: F1000 Prime Recommended

  2012

• Zhang, Min; Huang, Zheng; Yu, Binxun; Ji, Haitao.* New homogeneous high-throughput assays for inhibitors of β-catenin/Tcf protein-protein interactions.  Anal. Biochem.  2012, 424 (1), 57–63.

Review Articles

• Wang, Zhen;^† Li, Zilu;^† Ji, Haitao.* Direct targeting of β-catenin in the Wnt signaling pathway: current progress and perspectives. Med. Res. Rev. 2021, 41 (4), 2109–2129.
• Guo, Wenxing; Wisniewski, John A.; Ji, Haitao.* Hot spot-based design of small-molecule inhibitors for protein–protein interactions.  Bioorg. Med. Chem. Lett.  2014, 24 (11), 2546–2554. Commented by a popular drug discovery blog, In The Pipeline.

Book Chapters

• Ji, Haitao. Hot Spot-Based Design of Small-Molecule Inhibitors for Protein-Protein Interactions, in Targeting Protein-Protein Interactions by Small Molecules (eds. Chunquan Sheng and Guida Georg), 2018, pp 53-71, Springer, Singapore. doi: 10.1007/978-981-13-0773-7_3 (Print ISBN: 978-981-13-0772-0; Online ISBN: 978-981-13-0773-7).
• Teuscher, Kevin B.; Ji, Haitao. Protocol for fragment hopping, in Methods in Molecular Biology (Fragment-Based Methods in Drug Discovery, ed. Anthony E. Klon), 2015, volume 1289, pp 57–73. Springer, New York, USA. doi: 10.1007/978-1-4939-2486-8_6 (ISBN: 978-1-4939-2485-1). The book was commented by a popular drug discovery blog, Practical Fragments.
• Ji, Haitao; Silverman, Richard B. Case study 3: fragment hopping to design highly potent and selective neuronal nitric oxide synthase inhibitors, in Scaffold Hopping in Medicinal Chemistry (ed. Nathan Brown), 2013, pp 279–296. Wiley-VCH Verlag GmbH & Co. KGaA. Weinheim, Germany. doi: 10.1002/9783527665143.ch18 (ISBN: 978-3-527-33364-6).
• Ji, Haitao. Fragment-based drug design: considerations for good ADME properties, in ADMET for Medicinal Chemists: A Practical Guide (eds. Katya Tsaioun and Steven A. Kates), 2011, pp 417–485. John Wiley & Sons, Inc. Hoboken, NJ, USA. doi:10.1002/9780470915110.ch11 (ISBN: 978-0-470-48407-4).

Postdoctoral or Graduate Research (Selected Papers)

Northwestern University Working with Professor Richard B. Silverman

• Huang, He; Ji, Haitao; Li, Huiying; Jing, Qing; Labby, Kristin J.; Martásek, Pavel; Roman, Linda J.; Poulos, Thomas L.; Silverman Richard B. Selective monocationic inhibitors of neuronal nitric oxide synthase. Binding mode insights from molecular dynamics simulations.  J. Am. Chem. Soc.  2012, 134 (28), 11559–11572
• Ji, Haitao; Jing, Qing; Huang, Jinwen; Silverman, Richard B. Acid-facilitated debenzylation of N-Boc, N-benzyl double protected 2-aminopyridinomethyl pyrrolidine derivatives. Tetrahedron 2012, 68 (5), 1359-1366.
• Ji, Haitao; Delker, Silvia, L.; Li, Huiying; Martásek, Pavel; Roman, Linda, J.; Poulos, Thomas, L.; Silverman, Richard, B. Exploration of the active site of neuronal nitric oxide synthase by the design and synthesis of pyrrolidinomethyl 2-aminopyridine derivatives.  J. Med. Chem.  2010, 53 (21), 7804–7824.
• Delker, Silvia L.; Ji, Haitao; Li, Huiying; Jamal, Joumana; Fang, Jianguo; Xue, Fengtian; Silverman, Richard B.; Poulos, Thomas L. Unexpected binding modes of nitric oxide synthase inhibitors effective in the prevention of a cerebral palsy phenotype in an animal model.  J. Am. Chem. Soc.  2010, 132 (15), 5437–5442.
• Fang, Jianguo; Ji, Haitao; Lawton, Graham R.; Xue, Fengtian; Roman, Linda J.; Silverman Richard B. L337H Mutant of rat neuronal nitric oxide synthase resembles human neuronal nitric oxide synthase toward inhibitors.  J. Med. Chem.  2009, 52 (14), 4533–4537.
• Ji, Haitao; Tan, Sidhartha; Igarashi, Jotaro; Li, Huiying.; Derrick, Matthew; Martásek, Pavel; Roman, Linda J.; Vásquez-Vivar, Jeannette; Poulos, Thomas L.; Silverman, Richard B. Selective neuronal nitric oxide synthase inhibitors and the prevention of cerebral palsy.  Ann. Neurol.  2009, 65 (2), 209–217.
• Ji, Haitao; Li, Huiying; Martásek, Pavel; Roman, Linda J.; Poulos, Thomas L.; Silverman, Richard B. Discovery of highly potent and selective inhibitors of neuronal nitric oxide synthase by fragment hopping.  J. Med. Chem.  2009, 52 (3), 779–797.
• Igarashi, Jotaro; Li, Huiying; Jamal, Joumana; Ji, Haitao; Fang, Jianguo.; Lawton, Graham R.; Silverman, Richard B.; Poulos, Thomas L. Crystal structures of constitutive nitric oxide synthases in complex with de novo designed inhibitors.  J. Med. Chem.  2009, 52 (7), 2060–2066.
• Ji, Haitao; Stanton, Benjamin Z.; Igarashi, Jotaro; Li, Huiying; Martásek, Pavel; Roman, Linda J.; Poulos, Thomas L.; Silverman, Richard B. Minimal pharmacophoric elements and fragment hopping, an approach directed at molecular diversity and isozyme selectivity. Design of selective neuronal nitric oxide synthase inhibitors.  J. Am. Chem. Soc.  2008, 130 (12), 3900–3914.
• Clift, Michael; Ji, Haitao; Deniau, Gildas P.; O’Hagan, David; Silverman, Richard B. The enantiomers of 4-amino-3-fluorobutanoic acid as substrates for g-aminobutyric acid aminotransferase. Conformational probes for GABA binding.  Biochemistry  2007, 46 (48), 13819–13828.
• Ji, Haitao; Gómez-Vidal, José A.; Martásek, Pavel; Roman, Linda J.; Silverman, Richard B. Conformationally restricted dipeptide amides as potent and selective neuronal nitric oxide synthase inhibitors.  J. Med. Chem.  2006, 49 (21), 6254–6263.
• Ji, Haitao; Li, Huiying; Flinspach, Mack; Poulos, Thomas L.; Silverman, Richard B. Computer modeling of selective regions in the active site of nitric oxide synthases: implication for the design of isoform-selective inhibitors.  J. Med. Chem.  2003, 46 (26), 5700–5711.

Second Military Medical University, China

• Sheng, Chunquan; Ji, Haitao; Che, Xiaoyin; Miao, Zhenyuan; Yao, Jianzhong; Wang, Wenya; Guo, Wei; Lü, Jiaguo; Zhang Wannian. Homology modeling and molecular dynamics simulation of N-myristoyltransferase from protozoan parasites: active site characterization and insights into rational inhibitor design.  J. Comput.-Aided Mol. Des.  2009, 23 (6), 375–389.
• Sheng, Chunquan; Miao, Zhenyuan; Ji, Haitao; Yao, Jianzhong; Wang, Wenya; Che, Xiaoyin; Dong, Guoqiang; Lü, Jiaguo; Guo, Wei; Zhang, Wannian. A three-dimensional model of lanosterol 14a-demethylase from Cryptococcus neoformans: active site characterization and insights into azoles binding.  Antimicrob. Agents Chemother.  2009, 53 (8), 3487–3495.
• Yao, Bin; Ji, Haitao; Cao, Yongbin; Zhou, Youjun; Zhu, Jü; Lü, Jiaguo; Li, Yaowu; Chen, Jun; Zheng, Canhui; Jiang, Yuanying; Liang, Rongmei; Tang, Hui. Synthesis, antifungal activities of novel 2-aminotetralin derivatives.  J. Med. Chem.  2007, 50 (22), 5293–5300.
• Sheng, Chunquan; Zhang, Wannian; Ji, Haitao; Zhang, Min; Song, Yunlong; Xu, Hui; Zhu, Jie; Miao, Zhenyuan; Jiang, Qingfen; Yao, Jianzhong; Zhou, Youjun; Zhu, Jue; Lue, Jiaguo. Structure-based optimization of azole antifungal agents by CoMFA, CoMSIA, and molecular docking.  J. Med. Chem.  2006, 49 (8), 2512–2525.
• Ji, Haitao; Zhang, Wannian; Zhang, Min; Kudo, Makiko; Aoyama, Yuri; Yoshida, Yuzo; Sheng, Chunquan; Song, Yunlong; Yang, Song; Zhou, Youjun; Lü, Jiaguo; Zhu, Jü. Structure-based de novo design, synthesis and biological evaluation of nonazole inhibitors specific for lanosterol 14a-demethylase of fungi.  J. Med. Chem.  2003, 46 (4), 474–485.
• Ji, Haitao; Zhang, Wannian; Zhou, Youjun; Zhang, Min; Zhu, Jie; Song, Yunlong; Lü, Jiaguo; Zhu Jü. A three-dimensional model of lanosterol 14a-demethylase of Candida albicans and its interaction with azole antifungals.  J. Med. Chem.  2000, 43 (13), 2493–2505.