Structure-Based Inhibitor Design, Synthesis, and Chemical Biology

JI Research Group 

Ji Lab Is Accepting New Graduate Students

Professor Ji accepts new graduate students. The lab is located in H. Lee Moffitt Cancer Center & Research Institute. The graduate students in the Ji lab expect to receive training in rational drug design, synthetic organic chemistry, medicinal chemistry, chemical biology, and molecular and cell biology. Please apply here 

Ji Lab Is Looking for New Postdoc Fellows

POSTDOCTORAL POSITION available for the design and synthesis of selective small-molecule inhibitors of protein–protein interactions. Successful candidates must have a PhD in medicinal chemistry or synthetic organic chemistry. Strong background and experience in medicinal chemistry and/or organic synthesis is essential. Experience in relevant areas including medicinal chemistry and/or natural product synthesis is desirable. Submit CV and statement of research experience via email to Dr. Haitao (Mark) Ji ( Dr. Ji and the research team are in the Department of Drug Discovery. Recommendation letters will be requested when needed. Moffitt Cancer Center & Research Institute is an NCI-Designated Comprehensive Cancer Center.

Ji Lab Is Looking for New Postdoc Fellows

POSTDOCTORAL POSITION available for cancer biochemistry and chemical biology studies. We are looking for enthusiastic, highly self-motivated Ph.D. and/or M.D. fellows with strong laboratory skills in biochemistry and structural biology. The project involves the determination and characterization of highly selective small-molecule inhibitors for the crucial signaling pathways that are linked to tumorigenesis. Our ultimate goal is to provide novel targeted therapies for cancer. Submit CV and statement of research experience via email to Dr. Haitao (Mark) Ji ( Recommendation letters will be requested when needed. Moffitt Cancer Center & Research Institute is an NCI-Designated Comprehensive Cancer Center.

Zhen's paper on optimization of peptidomimetic β-catenin/Tcf inhbitors has just been accepted by J. Med. Chem.

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, Just Accepted.

Xiaowei's paper on Ruthenium (II)-catalyzed C–H allylation of alkene has been published by J. Org. Chem.

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.

Xiaowei's paper on Rhodium (III)-catalyzed C–H allylation of Indoles has been published by Org. Biomol. Chem.

Wu, Xiaowei; Ji, Haitao.Rhodium(III)-catalyzed C-H allylation of indoles with allyl alcohols via β-hydroxide elimination. Org. Biomol. Chem. 201816 (31), 5691-5698.

Xiaowei's paper on Rhodium-catalyzed [4 + 1] cyclization to synthesize quaternary carbon-containing heterocycles has been published by J. Org. Chem. 

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.

The optimization of beta-catenin/BCL9 inhibitors has been published by J. Med. Chem.

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.


Xiaowei's paper on Ruthenium (II)-catalyzed C–H allylation of Indoles has been published by Org. Lett.

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.

Two Series of Ji Lab Beta-Catenin/BCL9 Inhibitors Licensed 

Two series of beta-catenin/BCL9 inhibitors that were invented by the Ji lab have been licensed to VENN Therapeutics.  The News

Kevin's J. Med. Chem. paper published. This paper is featured as ACS Editors' Choice!

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 also recommended by F1000 faculty. Click the icon below to read the F1000 faculty recommendation.

Access the recommendation on F1000Prime

Ji Group Joined the Moffitt Cancer Center

Ji Lab has moved to the H. Lee Moffitt Cancer Center & Research Institute in Florida on August 1, 2016. The lab is located on the fourth floor of the Moffitt Research Center (MRC), and the room number is MRC4029B. Ji Lab will develop new tools/techniques for the rational design of protein-protein interaction (PPI) inhibitors and the application of newly developed tools/techniques to discover potent and selective PPI inhibitors.

Dr. Ji Received the Susan G. Komen Career Catalyst Research Grant!

This three-year research grant allows the Ji lab to develop selective small-molecule inhibitors for the beta-catenin/Tcf protein-protein interaction. The grant starts on September 1, 2016.

Ji Group Received the First Patent for Their Invention

Substituted 1H-indazol-1-ol analogs as inhibitors of beta catenin/Tcf protein-protein interactions. US 9,284,299 B2.

Jack's ACS Medicinal Chemistry Letters Paper Published

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.

Yongqiang's Chemical Science Paper Published

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.

Logan's JACS Paper Published

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.

Leon's J. Med. Chem. Paper Published

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.

Protocol for Fragment Hopping Published

Teuscher, Kevin B.; Ji, Haitao. Protocol for Fragment Hopping, in Methods in Molecular Biology, 2015, volume 1289, pp 57–73

Assay Peper for Catenin/B-Cell Lymphoma 9 Inhibitors Published

Zhang, Min; Wisniewski, John A.; Ji, Haitao. AlphaScreen Selectivity Assay for β-Catenin/B-Cell Lymphoma 9 Inhibitors. Anal. Biochem. 2015, 469, 43–53.

First Review Paper Published

Wenxing, Guo; John A. Wisniewski; Ji Haitao. Hot Spot-Based Design of Small-Molecule Inhibitors for Protein–Protein Interactions. Bioorg. Med. Chem. Lett., 2014, 24 (11), 2546–2554.

Undergraduate Research Presentations

Four undergraduate students (Sami Crouch, Danny Powell, Jessica Bones and Nina Eckstein) presented their works to academic feilds.

Click to see the pictures and read more details

DOD CDMRP Breast Cancer Research Grant

Dr. Ji received the Department of Defense (DOD) Congressionally Directed Medical Research Programs (CDMRP) Breast Cancer Research Program Breakthrough Award. This three-year grant starts in the summer of 2014.

Fourth Paper Published

Huang, Zheng; Zhang, Min; Burton, Shawn D.; Katsakhyan, Levon N.; and 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.

Highlight : Paper Recommended by the F1000 Faculty

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, has been recommended by the F1000 Faculty. Click the icon below to read the recommendation.

F1000Prime Recommended

Third Paper Published

Zhang, Min; Catrow, J. Leon and 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.

Second Paper Published

Yu, Binxun; Huang, Zheng; Zhang, Min; Dillard, Darren R. and 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.

Science Day

Dr. Ji gave a presentation on Computer-Aided Drug Design on University of Utah Science Day. Click to view pictures. 

Young investigator Award

05/15/2012: Dr. Ji won the Pulmonary Fibrosis Foundation Research Fund to Cure PF-Young investigator Award.

First Paper Published

Min Zhang, Zheng Huang, Binxun Yu, Haitao Ji. New Homogeneous High-Throughput Assays for Inhibitors of beta-Catenin/Tcf Protein-Protein Interaction. Anal. Biochem., 2012, 424, 57–63.

First Publication

Our first publication, a book chapter, titled "Fragment-Based Drug Design: Considerations for Good ADME Properties" has been published as Chapter 11 (pp 417-485) of ADMET for Medicinal Chemists: A Practical Guide (eds K. Tsaioun and S. A. Kates), 2011 by John Wiley & Sons, Inc. It is currently available.


2014 Jun. Group trip to Moab. See more photos.

2013 Aug. End of summer BBQ in Millcreek Canyon! More photos

2012 Jun. Group picnic giving welcome to new members doing summer research. See photos

2012 Apr. As Toni and Anne are going back to Germany, Michelle is graduating soon,. Mark hosted a BBQ party. More photos