Education B.S., Nanjing University, 1993-1997 Advisor: Yun Lu M.S., Nanjing University, 1997-2000 Advisor: Yun Lu Ph.D., Washington University in St. Louis, 2002-2006 Advisor: John-Stephen A. Taylor Postdoctoral Associate, Yale University, 2007-2009 Advisor: Andrew D. Hamilton Affiliations and Positions Distinguished University Professor, Department of Chemsitry, USF, 2024- USF Preeminent Professor, Department of Chemsitry, USF, 2020- Director, Center for Molecular Diversity in Drug Design, Discovery and Development (CMD5), USF, 2019- Professor, Department of Chemsitry, USF, 2018- Associate professor, Department of Chemsitry, USF, 2015-2018 Assistant professor, Department of Chemsitry, USF, 2009-2015 Member, American Peptide Society, 2014- Member, Moffitt Cancer Center & Research Institute, 2009- Member, American Chemical Society, 2005-

AApeptide Folding Structure-Based Design Combinatorial Screening Supramolecular Chemistry

Anna Kharitonova, Rekha S Patel, Brenna Osborne, Meredith Krause-Hauch, Ashley Lui, Gitanjali Vidyarthi, Sihao Li, Jianfeng Cai, Niketa A Patel.* NPC86 Increases LncRNA Gas5 in vivo to Improve Insulin Sensitivity and Metabolic Function in Diet-Induced Obese Diabetic Mouse Model. Int. J. Mol. Sci. 2025, accepted. Bo Huang, Sihao Li, Cong Pan, Fangzhou Li, Lukasz Wojtas, Qiao Qiao, Timothy H. Tran, Laurent Calcul, Wenqi Liu, Chenfeng Ke,* Jianfeng Cai.* Proline-Based Tripodal Cages with Guest-Adaptive Features for Capturing Hydrophilic and Amphiphilic Fluoride Substances. Nat. Commun. 2025, 16, 3226. Heng Liu, Xue Zhao, Jianyu Chen, Yu Yu Win, and Jianfeng Cai.* Unnatural foldamers as inhibitors of Aβ aggregation via stabilizing Aβ helix. Chem. Commun. 2025, 61, 4586–4594. Jarais Fontaine and Jianfeng Cai.* Recent exploration of γ-AApeptide based antimicrobial peptide mimics as potential therapeutics towards drug-resistant bacteria. Exploration Drug Sci. 2025, 3:100888. Yafeng Wang,+ Xueqing Hu,+ Shriya Pandey,+ Ujjwol Khatri, Tao Shen, Vivek Subbiah, Blaine H. M. Mooers, Ting Chao, Shaohui Wang, Huaxuan Yu, Xingmin Sun, Jie Wu,* and Jianfeng Cai.* Targeting oncogenic RET kinase by simultaneously inhibiting kinase activity and degrading the protein. J. Med. Chem. 2025, 68, 1, 81–94. Haohui Ye and Jianfeng Cai.* Cationic Catalysts as a New Strategy to Catalyze N-Carboxyanhydrides Polymerization. ACS Central Sci., 2025, accepted. Jinhua Xie,+ Shahedul Islam,+ Le Wang,* Xiaojing Zheng, Mengsheng Xu, Xiqi Su, Shaohua Huang, Logan Suits, Guang Yang, Prahathees Eswara, Jianfeng Cai, Li-June Ming.* A tale of two old drugs tetracycline and salicylic acid with new perspectives—Coordination chemistry of their Co(II) and Ni(II) complexes, redox activity of Cu(II) complex, and molecular interactions. J. Inorg. Biochem. 2025, 262, 112757. Wei Jiang, Jiayan Chen, Haifeng Wang, Aiqi Xue, Xinyang Zhang, Jichi Guan, Lulu Wei, Jianfeng Cai,* Yong Hu,* and Dan Liu.* Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as VEGFR2 Kinase Inhibitors for Tumor Treatment. Chem. Res. Chin. Univ. 2024, 41(1), 66―78. Zhikai Li, Yu Yan, Zhi Chen, Runxu Tang, Ningxu Han, Runlin Han, Fang Fang, Jichun Jiang, Lei Hua, Xiujun Yu, Ming Wang, Jianfeng Cai, Haiyang Li, Heng Wang* and Xiaopeng Li.* Multi-Dimensional Decryption of Metallopolymer at Single-Chain Level. CCS Chem. 2025, accepted. Canjia Zhai, Ethan Cross Zulueta, Alexander Mariscal, Chengkai Xu, Yunpeng Cui, Xudong Wang, Huang Wu, Carson Doan, Lukasz Wojtas, Haixin Zhang, Jianfeng Cai, Libin Ye, Kun Wang, Wenqi Liu.* From Small Changes to Big Gains: Pyridinium-Based Tetralactam Macrocycle for Enhanced Sugar Recognition in Water. Chem. Sci. 2024, 15, 19588-19598. Ying Feng, YongChao Zhu, Tian Chen, Pengcheng Li, Bingjie Liu, Jianfeng Cai,* Wenjie Liang,* and Hai Xu.* Green and efficient preparation and application of weakly crystalline TiO2 with high catalytic activity. New J. Chem., 2024, 48, 515-519. Ruixuan Gao, Menglin Xue, Ning Shen, Xue Zhao, Justin C. Zhang, Chuanhai Cao, and Jianfeng Cai.* Development of low-toxicity antimicrobial polycarbonates bearing lysine residues. Chem. Eur. J. 2024, e202402302. Yuwei Zheng, Jiaying Chi, Jiayu Ou, Ling Jiang, Liqing Wang, Rui Luo, Yilang Yan, Zejun Xu, Tingting Peng, Jianfeng Cai, Chuanbin Wu, Peng Teng,* Guilan Quan,* Chao Lu.* Imidazole-Rich, Four-Armed Host-Defense Peptidomimetics as Promising Narrow-Spectrum Antibacterial Agents and Adjuvants against Pseudomonas Aeruginosa Infections. Adv. Healthcare Mater., 2024, 2400664. Tengyue Jian,+ Minghui Wang,+ Jeevapani Hettige, Yuhao Li, Lei Wang, Ruixuan Gao, Wenchao Yang, Renyu Zheng, Shengliang Zhong, Marcel D. Baer, Aleksandr Noy, James. J. De Yoreo, Jianfeng Cai,* Chun-Long Chen.* Self-assembling and pore-forming peptoids as novel antimicrobial biomaterials. ACS Nano, 2024, 18, 23077–23089. Shannon J. Ho, Dale Chaput, Rachel G. Sinkey, Amanda H. Garces, Erika P. New, Maja Okuka, Peng Sang, Sefa Arlier, Nihan Semerci, Thora S. Steffensen, Thomas J. Rutherford, Angel E. Alsina, Jianfeng Cai, Matthew L. Anderson, Ronald R. Magness, Vladimir N. Uversky, Derek A. T. Cummings & John C. M. Tsibris. Cell Commun. Signaling 2024, 22, 221. Xue Zhao, Heng Liu, Justin C. Zhang, Jianfeng Cai.* Helical Sulfonyl-γ-AApeptides in the Inhibition of HIV-1 Fusion and HIF-1α Signaling. RSC Med. Chem. 2024, 15, 1418-1423. Heng Liu, Yunpeng Cui, Xue Zhao, Lulu Wei, Xudong Wang, Ning Shen, Timothy Odom, Xuming Li, William Lawless, Kanchana Karunarathne, Martin Muschol, Wayne Guida, Chuanhai Cao, Libin Ye, and Jianfeng Cai.* Helical sulfonyl-γ-AApeptides modulating Aβ oligomerization and cytotoxicity by recognizing Aβ helix. Proc. Natl. Acad. Sci. U. S. A. 2024, 121, 6, e2311733121. Menglin Xue,+ Soumyadeep Chakraborty,+ Ruixuan Gao,+ Shaohui Wang, Meng Gu, Ning Shen, Lulu Wei, Chuanhai Cao, Xingmin Sun,* and Jianfeng Cai.* Antimicrobial Guanidinylate Polycarbonates Show Oral In Vivo Efficacy Against Clostridioides difficile. Adv. Healthcare Mater. 2024, 2303295 Prakash Jadhav,+ Bo Huang,+ Jerzy Osipiuk,+ Xiaoming Zhang, Haozhou Tan, Christine Tesar, Michael Endres, Robert Jedrzejczak, Bin Tan, Xufang Deng, Andrzej Joachimiak,* Jianfeng Cai,* Jun Wang.* Structure-based design of SARS-CoV-2 papain-like protease inhibitors. Eur. J. Med. Chem. 2024, 264, 116011. Xiaomin Guo,+ Xiaokang Miao,+ Yingying An, Tiantian Yan, Yue Jia, Bochuan Deng, Jianfeng Cai, Wenle Yang, Wangsheng Sun,* Rui Wang,* Junqiu Xie.* Novel antimicrobial peptides modified with fluorinated sulfono-γ-AA having high stability and targeting multidrug-resistant bacteria infections. Eur. J. Med. Chem. 2024, 264, 116001. Wenhao Wang, Chao Lu,* , Zhengwei Huang,* , Lei Shu, Jianfeng Cai, Chuanbin Wu and Xin Pan. A Bibliometric Study on Nanomedicines as Melanoma Therapeutics: Clinical Translation is Urgent. Oncol. Adv. 2023, 1, 25-30. Zhanpeng Zhang, Shuai Lu,* Xiujun Yu, Lei Hua, Weiguo Wang, Menglin Xue, Jianfeng Cai, Heng Wang,* Xiaopeng Li. Construction of Metallo-Helicoids via Intermolecular Coordination with High Antimicrobial Activity. Chem. Commun. 2023, 59, 13022-13025. Yuqing Tong,+ Meng Gu,+ Xingyu Luo, Haifeng Qi, Wei Jiang, Yu Deng, Lulu Wei, Jun Liu, Yin Ding,* Jianfeng Cai,* Yong Hu.* An engineered nanoplatform cascade to relieve extracellular acidity and enhance resistance-free chemotherapy. J. Control. Release. 2023, 363, 562-573. Wei Jiang,+ Sami Abdulkadir,+ Xue Zhao,+ Peng Sang, Anastasia Tomatsidou, Xiujun Zhang, Yu Chen, Laurent Calcul, Xingmin Sun, Feng Cheng,* Yong Hu,* Jianfeng Cai.* Inhibition of Hypoxia-Inducible Transcription Factor (HIF-1α) Signaling with Sulfonyl-γ-AApeptide Helices. J. Am. Chem. Soc. ASAP. Songyi Xue,+ Wei Xu,+* Lei Wang, Ling Xu, Laurent Calcul, Peng Teng, Lu Lu, Shibo Jiang,* and Jianfeng Cai.* Rational Design of Sulfonyl-γ-AApeptides as Highly Potent HIV-1 Fusion Inhibitors with Broad-spectrum Activity. J. Med. Chem. ASAP. Ali Azmy,+ Xue Zhao,+ Giasemi K. Angeli, Claire Welton, Parth Raval, Lukasz Wojtas, Nourdine Zibouche, G. N. Manjunatha Reddy, Pantelis N. Trikalitis, Jianfeng Cai, and Ioannis Spanopoulos.* One Year Water Stable and Porous Bi(III) Halide Semiconductor with Broad Spectrum Antibacterial Performance. ACS App. Mater. Inter. ASAP. Peng Sang,* Jianfeng Cai.* Unnatural Helical Peptidic Foldamers as Protein Segment Mimics. Chem. Soc. Rev. 2023, 52, 4843-4877. Seid Yimer Abate,+ Ziqi Yang,+ Surabhi Jha, Jada Emodogo, Guorong Ma, Zhongliang Ouyang, Shafi Muhammad, Nihar Pradhan, Xiaodan Gu, Derek Patton, Dawen Li, Jianfeng Cai,* and Qilin Dai.* Promoting large area slot-die coated perovskite solar cells performance and reproducibility by acid-based sulfono-γ-AApeptide. ACS Appl. Mater. Inter. 2023, 15, 21, 25495–25505. Hongtao Kong,+ Shangshang Qin,+ Dachao Yan, Boyuan Shen, Tingting Zhang, Meng Wang, Sen Li, Maxwell Ampomah-Wireko, Mengmeng Bai, En Zhang,* Jianfeng Cai.* Development of aromatic-linked diamino acid antimicrobial peptide mimics with low hemolytic toxicity and excellent activity against methicillin-resistant Staphylococcus aureus (MRSA). J. Med. Chem. 2023, accepted. Songyi Xue,+ Wei Xu,+* Lei Wang, Xinling Wang, Qianyu Duan, Laurent Calcul, Shaohui Wang, Wenqi Liu, Xingmin Sun, Lu Lu,* Shibo Jiang,*, and Jianfeng Cai.* An HR2-mimicking sulfonyl-γ-AApeptide is a potent pan-coronavirus fusion inhibitor with strong blood-brain barrier permeability, long half-life and promising oral bioavailability. ACS Central. Sci. 2023, accepted. Diego Alem, Xinrui Yang, Francisca Beato, Bhaswati Sarcar, Alexandra F. Tassielli, Ruifan Dai, Tara L. Hogenson, Margaret A. Park, Kun Jiang, Jianfeng Cai, Yu Yuan, Martin E. Fernandez-Zapico, Aik Choon Tan, Jason B. Fleming, Hao Xie.* Translational relevance of SOS1 targeting for KRAS‐mutant colorectal cancer. Mol. Carcinogenesis, 2023, Accepted. Yafeng Wang, Menglin Xue, Ruixuan Gao, Soumyadeep Chakraborty, Shaohui Wang, Xue Zhao, Meng Gu, Chuanhai Cao, Xinmin Sun, Jianfeng Cai.* Short lipidated dendrimeric γ-AApeptides as new antimicrobial peptidomimetics. Int. J. Mol. Sci., 2023, 24, 7, 6407. Lei Wang,+ Chunlong Ma,+ Michael Dominic Sacco,+ Songyi Xue, Mentalla Mahmoud, Laurent Calcul, Yu Chen,* Jun Wang,* and Jianfeng Cai.* Development of the Safe and Broad-Spectrum Aldehyde and Ketoamide Mpro inhibitors Derived from the Constrained α, γ-AA Peptide Scaffold. Chem. Eur. J. 2023, ASAP. Meng Gu,+ Ying Yu,+ Menglin Xue, Jianxiong Jiang,* Jianfeng Cai.* The discovery of cyclic γ-AApeptides as the promising ligands targeting EP2. Bioorg. Med. Chem. Lett. 2023, 87, 129255. Peng Teng,* Haodong Shao, Bo Huang, Junqiu Xie, Sunliang Cui,* Kairong Wang,* Jianfeng Cai.* Small Molecular Mimetics of Antimicrobial Peptides as a Promising Therapy to Combat Bacterial Resistance. J. Med. Chem. 2023, 66, 4, 2211–2234. Oksana Fihurka, Yanhong Wang, Yuzhu Hong, Xiaoyang Lin, Ning Shen, Haiqiang Yang, Breanna Brown, Marcus Mommer, Tarek Zieneldien, Yitong Li, Janice Kim, Minghua Li, Jianfeng Cai, Qingyu Zhou,* Chuanhai Cao.* Multi-targeting intranasal nanoformulation as a therapeutic for Alzheimer's disease. Biomolecules, 2023, 13, 232. Ruixuan Gao, Xuming Li, Menglin Xue, Ning Shen, Minghui Wang, Jingyao Zhang, Chuanhai Cao, and Jianfeng Cai.* Development of Lipidated Polycarbonates with Broad-Spectrum Antimicrobial Activity. Biomater. Sci. 2023, 11, 1840-1852. Xiaoqian Feng, Dongyi Xiana, Jintao Fu, Rui Luo, Wenhao Wang, Yuwei Zheng, Qing He, Zhan Ouyang, Shaobin Fang, Wancong Zhang, Daojun Liu, Shijie Tang, Guilan Quan, Jianfeng Cai, Chuanbin Wu, Chao Lu,* Xin Pan.* Four-armed host-defense peptidomimetics-augmented vanadium carbide MXene-based microneedle array for efficient photo-excited bacteria-killing. Chem. Eng. J. 2023, 456, 141121. Rekha S. Patel, Ashley Lui, Charles Hudson, Lauren Moss, Robert Sparks, Shannon E. Hill, Yan Shi, Jianfeng Cai, Laura J. Blair, Paula Bickford, Niketa A. Patel.* Small molecule targeting long noncoding RNA GAS5 administered intranasally improves neuronal insulin signaling and decreases neuroinflammation in an aged mouse model. Sci. Rep. 2023, 13, 373. Seid Yimer Abate,+ Ziqi Yang,+ Surabhi Jha, Guorong Ma, Zhongliang Ouyang, Haixin Zhang, Shafi Muhammad, Nihar Pradhan, Xiaodan Gu, Derek Patton, Kun Wang, Dawen Li, Jianfeng Cai,* Qilin Dai.* Room Temperature Slot-Die Coated Perovskite Layer Modified with sulfonyl-γ-AApeptide for High Performance Perovskite Solar Devices. Chem. Eng. J. 2023, 457, 141199. Li Zhou,+ In Ho Jeong,+ Songyi Xue, Menglin Xue, Lei Wang, Sihao Li, Ruochuan Liu, Geon Ho Jeong, Xiaoyu Wang, Jianfeng Cai,* Jun Yin,* Bo Huang.* Inhibition of the ubiquitin transfer cascade by peptidomimetic foldamer mimicking E2 N-terminal-helix. J. Med. Chem. 2023, 66, 1, 491–502. Xueying Ge, Fangchao Jiang, Minghui Wang, Meng Chen, Yiming Li, Joshua Phipps, Jianfeng Cai, Jin Xie, Jane Ong, Viktor Dubovoy, James G. Masters, Long Pan,* Shengqian Ma.* Naringin@Metal-Organic Framework as a Multifunctional Bio-platform. ACS Applied Mater. Interface. 2023, 15, 1, 677–683. Pengcheng Li, Xiaohuan Chen, Cui Guo, Huijing Zou, Ziyi Chen, Bingjie Liu, Wenjie Liang,* Jianfeng Cai,* Hai Xu.* A Logic Fluorescent Chemosensor Based on Eu3+ Functionalized Cd-MOFs for Sensing Fe3+ and Cu2+ Synchronously. Eur. J. Inorg. Chem. 2023, ASAP. Xiaomin Guo, Tiantian Yan, Jing Rao, Yingying An, Xin Yue, Xiaokang Miao, Rui Wang, Wangsheng Sun,* Jianfeng Cai,* and Junqiu Xie.* Novel Feleucin-K3-derived peptides modified with sulfono-γ-AA building blocks targeting Pseudomonas aeruginosa and MRSA infections. J. Med. Chem. 2023, 66, 2, 1254-1272. Yan Shi,+ Candy Lee,+ Peng Sang, Zaid Amso, David Huang, Weixia Zhong, Meng Gu, Lulu Wei, Vân T. B. Nguyen-Tran, Jingyao Zhang, Weijun Shen,* Jianfeng Cai.* α/Sulfono-γ-AA peptide hybrids agonist of GLP-1R with prolonged action both in vitro and in vivo. Acta Pharmaceutica Sinica B, 2023, 1648-1659. Yujia Bian, Diego Alem, Francisca Beato, Tara L. Hogenson, Xinrui Yang, Kun Jiang, Jianfeng Cai, Wen Wee Ma, Martin Fernandez-Zapico, Aik Choon Tan, Nicholas J. Lawrence, Jason B. Fleming, Yu Yuan*, Hao Xie.* Development of SOS1 inhibitor-based degraders to target KRAS-mutant colorectal cancer. J. Med. Chem. 2022, 65, 24, 16432–16450. Songyi Xue,+ Xinling Wang,+ Lei Wang, Wei Xu, Shuai Xia, Lujia Sun, Shaohui Wang, Ning Shen, Ziqi Yang, Bo Huang, Sihao Li, Chuanhai Cao, Laurent Calcul, Xingmin Sun, Lu Lu,* Jianfeng Cai,* and Shibo Jiang.* A novel cyclic γ-AApeptide-based long-acting pan-coronavirus fusion inhibitor with potential oral bioavailability by targeting two sites in spike protein. Cell. Dis. 2022, 8, 88. Jie Zhong, Yuegui Guo, Shaoyong Lu, Kun Song, Ying Wang, Li Feng, Zhen Zheng, Qiufen Zhang, Jiacheng Wei, Peng Sang, Yan Shi, Jianfeng Cai, Guoqiang Chen, Chen-Ying Liu,* Xiuyan Yang,* and Jian Zhang.* Rational design of a sensitivity-enhanced tracer for discovering efficient APC-Asef inhibitors .Nat. Commun. 2022, 13(1):4961. Songyi Xue,+ Lei Wang,+ Jianfeng Cai.* Sulfono-γ-AApeptides as protein helical domain mimetics to manipulate the angiogenesis.ChemBioChem 2022, 23, e202200298. Xing Zhang,+ Minghui Wang,+ Xiaodi Zhu, Yan Peng, Tiwei Fu, Chang-Hua Hu, Jianfeng Cai,* Guojian Liao.* Development of lipo-γ-AA peptides as potent antifungal agents.J. Med. Chem. 2022, 65, 11, 8029–8039. Feng Li,+ Liming Lin,+ Jiaying Chi, Hui Wang, Minqun Du, Disang Feng, Liqing Wang, Rui Luo, Hangping Chen, Guilan Quan, Jianfeng Cai, Xin Pan, Chuanbin Wu, Chao Lu.* Guanidinium-Rich Lipopeptide Functionalized Bacteria-Absorbing Sponge as an Effective Trap-and-Kill System for the Elimination of Focal Bacterial Infection.Acta Biomaterialia 2022, 148, 106-118. Peng Sang, Yan Shi, Lulu Wei, and Jianfeng Cai.* Helical Sulfono-γ-AApeptides with Predictable Functions in Protein Recognition. RSC Chem. Biol. 2022, 3, 805. Yanhong Wang, Yuzhu Hong, Jiyu Yan, Breanna Brown, Xiaoyang Lin, Xiaolin Zhang, Ning Shen, Minghua Li, Jianfeng Cai, Marcia Gordon, David Morgan, Qingyu Zhou,* and Chuanhai Cao.* Low-Dose Delta-9-Tetrahydrocannabinol as Beneficial Treatment for Aged APP/PS1 Mice. Int. J. Mol. Sci. 2022. 23, 5, 2757. Wei Jiang,+ Lulu Wei,+ Bing Chen, Xingyu Luo, Peipei Xu, Jianfeng Cai, and Yong Hu.* Platinum Prodrug Nanoparticles Inhibiting Tumor Recurrence and Metastasis by Concurrent Chemoradiotherapy. J. Nano. Biotechnol. 2022. 20:129. Jintao Fu,Ting Liu, Xiaoqian Feng, Yixian Zhou, Minglong Chen, Wenhao Wang, Yiting Zhao, Chao Lu, Guilan Quan, Jianfeng Cai, Xin Pan*, Chuanbin Wu. Perfect Pair: Stabilized Black Phosphorous Nanosheets Engineering with Antimicrobial Peptides for Robust Multi-Drug Resistant Bacteria Eradication. Adv Healthc Mater. 2022. e2101846. Peng Teng* and Jianfeng Cai.* Using Proteomimetics to Switch Angiogenic Signaling. Acta Pharmaceutica Sinica B 2022. 1534-1535. Bo Huang,+ Li Zhou,+ Ruochuan Liu,+ Lei Wang, Songyi Xue, Yan Shi, Geon Ho Jeong, In Ho Jeong, Sihao Li, Jun Yin,* Jianfeng Cai.* Activation of E6AP/UBE3A-Mediated Protein Ubiquitination and Degradation Pathways by a Cyclic Gamma-AApeptide. J. Med. Chem. 2022, 65, 2497-2506. Sami Abdulkadir,+ Chunpu Li,+ Wei Jiang,+ Xue Zhao, Peng Sang, Lulu Wei, Yong Hu,* Qi Li,* and Jianfeng Cai.* Modulating Angiogenesis by Proteomimetics of Vascular Endothelial Growth Factor. J. Am. Chem. Soc., 2022, 144, 1, 270–281. Lulu Wei and Jianfeng Cai.* Novel Peptides and Peptidomimetics in Drug Discovery. Acta Pharmaceutica Sinica B, 2021, 2606-2608. Maochao Zheng, Huanchang Lina, Wancong Zhang, Shijie Tang,* Daojun Liu,* and Jianfeng Cai.* Poly(L-ornithine)-grafted zinc phthalocyanines as dual-functional antimicrobial agents with intrinsic membrane damage and photothermal ablation capacity. ACS Infect. Dis. 2021, 7, 10, 2917–2929. Peng Sang,+ Hongxiang Zeng,+ Candy Lee,+ Yan Shi, Minghui Wang, Cong Pan, Lulu Wei, Chenglong Huang, Mingjun Wu, Weijun Shen,* Xi Li,* and Jianfeng Cai.* α/sulfono-γ-AApeptide Hybrid Analogues of Glucagon with Enhanced Stability and Prolonged in vivo Activity. J. Med. Chem. 2021, 64, 18, 13893–13901. Mengmeng Zheng,+ Chunpu Li,+ Mi Zhou,+ Ru Jia, Gang Cai, Fengyu She, Lulu Wei, Shaohui Wang, Jie Yu, Dingyan Wang, Laurent Calcul, Xingmin Sun, Xiaomin Luo, Feng Cheng, Qi Li,* Yan Wang,* and Jianfeng Cai.* Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR. J. Med. Chem. 2021, 64, 15, 11219-11228. Wei Jiang, Xingyu Luo, Lulu Wei, Shanmei Yuan, Jianfeng Cai,* Xiqun Jiang,* and Yong Hu.* The Sustainability of Energy Conversion Inhibition for Tumor Ferroptosis Therapy and Chemotherapy. Small, 2021, 17, 38, 2102695. Mengmeng Zheng,+ Chunpu Li,+ Mi Zhou,+ Ru Jia, Fengyu She, Lulu Wei, Feng Cheng, Qi Li, * Jianfeng Cai* and Yan Wang.* Peptidomimetic-based antibody surrogate for HER2. Acta Pharmaceutica Sinica B, 2021, 2645-2654. Yingru Zhang,+ Chunpu Li,+ Ru Jia,+ Ruixuan Gao, Yiyang Zhao, Qing Ji, Jianfeng Cai,* Qi Li,* and Yan Wang.* PEG-poly(amino acid)s/EpCAM aptamer multifunctional nanoparticles arrest the growth and metastasis of colorectal cancer. Biomater. Sci. 2021, 9, 3705-3717. Song Qing, Han Zhifen, Xinnan Wu, Yan Wang, Lihong Zhou, Liu Yang, Ningning Liu, Hua Sui, Jianfeng Cai, Qing Ji,* Li Qi.* β-arrestin1 promotes colorectal cancer metastasis through GSK-3β/β-catenin signaling-mediated epithelial-to-mesenchymal transition. Frontiers Cell Develop. Biol. 2021, 9, 650067. Yan Shi, Peng Sang and Jianfeng Cai.*. Discovery of α‑Helix-Mimicking Sulfono-γ-AApeptides as p53−MDM2 inhibitors. Future. Med. Chem. 2021, 12, 1021-1023. Minghui Wang,+ Xiaoqian Feng,+ Ruixuan Gao, Peng Sang, Xin Pan, Lulu Wei, Chao Lu,* Chuanbin Wu,* Jianfeng Cai.* Modular Design of Membrane Active Antibiotics: From Macromolecular Antimicrobials to Small Scorpion-like Peptidomimetics. J. Med. Chem. 2021, 64, 14, 9894-9905. Peng Teng,*,+ Mengmeng Zheng,+ Darrell Cole Cerrato, Yan Shi, Mi Zhou, Songyi Xue, Wei Jiang, Lukasz Wojtas, Li-June Ming, Yong Hu,* Jianfeng Cai.* The Folding Propensity of α/Sulfono-γ-AA Peptidic Foldamers with Both Left- and Right-Handedness. Commun. Chem. 2021, 58, 4. Lulu Wei,+ Ruixuan Gao,+ Minghui Wang,+ Yafeng Wang, Yan Shi, Meng Gu and Jianfeng Cai.* Dimeric Lipo-α/sulfono-γ-AA Hybrid Peptides as Broad-Spectrum Antibiotic Agents. Biomater. Sci. 2021, 9, 3410–3424. Yin Shi, Xiaoqian Feng, Jing Wang, Limin Lin, Biyuan Wu, Guilin Zhou, Feiyuan Yu, Qian Xu, Daojun Liu, Guilan Quan, Chao Lu,* Xin Pan,* Jianfeng Cai,* Chuanbin Wu.* Virus-Inspired Surface-Nanoengineered Antimicrobial Liposome: A potential System to Simultaneously Achieve High Activity and Selectivity. Bioactive Mat. 2021, 6, 3207-3217. Maochao Zheng, Miao Pan, Wancong Zhang, Huanchang Lin,Shenlang Wu, Chao Lu,* Shijie Tang,* Daojun Liu,* Jianfeng Cai.* Poly(α-L-lysine)-based nanomaterials for versatile biomedical applications: Current advances and perspectives. Bioactive Mat. 2021, 6, 1878-1909. Jianfeng Cai* and Ruihui Liu.* Introduction to Antibacterial Biomaterials. Biomater. Sci. 2020, 8, 6812-6813. Qing Song, Liu Yang, Zhifen Han, Xinnan Wu, Ruixiao Li, Lihong Zhou, Ningning Liu, Hua Sui, Jianfeng Cai, Yan Wang, Qing Ji,* and Qi Li.* Tanshinone IIA Inhibits Epithelial-to-Mesenchymal Transition Through Hindering β-Arrestin1 Mediated β-Catenin Signaling Pathway in Colorectal Cancer. Front. Pharmacol. 2020, 11, 586616. Yan Shi,+ Peng Sang,+ Junhao Lu,+ Pirada Higbee,+ Lihong Chen, Leixiang Yang, Timothy Odom, Gary Daughdrill,* Jiandong Chen,* and Jianfeng Cai.* Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein−Protein Interactions. J. Med. Chem. 2020, 63, 21, 13187–13196. Minghui Wang, Ruixuan Gao, Mengmeng Zheng, Peng Sang, Chunpu Li, En Zhang, Qi Li, and Jianfeng Cai.* Development of Bis-Cyclic Imidazolidine-4-one Derivatives as Potent Antibacterial Agents. J. Med. Chem. 2020, 63, 24, 15591-15602. Peng Sang,+ Yan Shi,+ Bo Huang, Songyi Xue, Timothy Odom, and Jianfeng Cai.* Sulfono-γ-AApeptides as helical mimetics: Crystal structures and applications. Acc. Chem. Res. 2020, 53, 10, 2425–2442. Runzhe Song, Yue Wang, Minghui Wang, Ruixuan Gao, Teng Yang, Song Yang, Cai-Guang Yang, Yongsheng Jin, Siyuan Zou, Jianfeng Cai,* Renhua Fan,* Qiuqin He.* Design and synthesis of novel desfluoroquinolone-aminopyrimidine hybrids as potent anti-MRSA agents with low hERG activity. Bioorg. Chem. 2020, 104176. Miao Pan,+ Chao Lu, Maochao Zheng, Wen Zhou, Fuling Song, Weidong Chen, Fen Yao, Daojun Liu,* and Jianfeng Cai.* Unnatural Amino Acid-Based Star-Shaped Poly(L-ornithine)s as Emerging Long-Term and Biofilm-Disrupting Antimicrobial Peptides to Treat Pseudomonas aeruginosa Infected Burn Wounds. Adv. Healthcare. Mat., 2020, 9, 19, 2000647. Ge Song, Haiqiang Yang, Ning Shen, Phillip Pham, Breanna Brown, Xiaoyang Lin,Yuzhu Hong, Paul Sinu, Jianfeng Cai, Xiaopeng Li, Michael Leon, Marcia Gordon, David Morgan, Sai Zhang, and Chuanhai Cao.* An Immunomodulatory Therapeutic Vaccine Targeting Oligomeric Amyloid Beta. J. Alz. Dis., 2020, 77, 4, 1639-1653. Peng Sang,+ Yan Shi,+ Pirada Higbee,+ Minghui Wang, Sami Abdulkadir, Junhao Lu, Gary W. Daughdrill,* Jiandong Chen,* and Jianfeng Cai.* Rational Design and Synthesis of Right-Handed D-Sulfono-γ-AApeptide Helical Foldamers as Potent Inhibitors of Protein-Protein Interactions. J. Org. Chem. 2020, 85, 10552-10560. Chengming Fu, Tian Chen, Tile Xiao, Yuecai Song, Timothy Odom, Wenjie Liang,* Jianfeng Cai,* Hai Xu.* Formaldehyde Gas Adsorption in High‐Capacity Silver‐Nanoparticle‐Loaded ZIF‐8 and UiO‐66 Frameworks. ChemistrySelect, 2020, 5987-5992. Hao Liu, Shijie Yi, Yunfeng Wu, Han Wu, Jinrong Zhou, Wenjie Liang,* Jianfeng Cai,* and Hai Xu.* An efficient Co-N/C electrocatalyst for oxygen reduction facilely prepared by tuning cobalt species content. Int. J. Hydro. Energy 2020, 16105-16113. Minghui Wang, Ruixuan Gao, Peng Sang, Tomothy Odom, Mengmeng Zheng, Yan Shi, Hai Xu, Chuanhai Cao and Jianfeng Cai.* Dimeric γ-AApeptides with Potent and Selective Antibacterial Activity. Front. Chem. 2020, 8, 441. Jing Wang,+ Chao Lu,+ Yin Shi, Xiaoqian Feng, Biyuan Wu, Guilin Zhou, Guilan Quan, Xin Pan,* Jianfeng Cai,* and Chuanbin Wu.* Structural Superiority of Guanidinium-Rich Four-Armed Copolypeptides: Role of Multiple Peptide-Membrane Interactions in Enhancing Bacterial Membrane Perturbation and Permeability. ACS. Appl. Mater. Inter. 2020, 12, 16, 18363-18374. Yan Shi,+ Peng Sang,+ Guangqiang Yin, Ruixuan Gao Xiao Liang, Robert Brzozowski, Prahathees Eswara, Timothy Odom, Youxuan Zheng,* Xiaopeng Li,* and Jianfeng Cai.* Aggregation-Induced Emissive and Circularly Polarized Homogeneous Sulfono-γ-AApeptide Foldamers. Adv. Opt. Mater. 2020, 8, 1902122. Peng Sang,+ Zhihong Zhou,+ Yan Shi, Candy Lee, Zaid Amso, David Huang, Timothy Odom, Vân T.B. Nguyen-Tran, Weijun Shen,* and Jianfeng Cai.* The Activity of Sulfono-γ-AApeptide Helical Foldamers That Mimic GLP-1. Sci. Adv. 2020, 6, 20, eaaz4988. Minghui Wang, Timothy Odom, and Jianfeng Cai.* Challenges in the development of next-generation antibiotics: Opportunities of small molecules mimicking mode of action of host-defense peptides. Exp. Opin. Ther. Pat. 2020, 303-305, De-Yun Cui, Hong-Tao Kong, Yi Yang, Jianfeng Cai, Bo-Yuan Shen, Da-chao Yan, Xiu-Juan Zhang, Ying-Long Qu, Meng-Meng Bai, En Zhang.* Asymmetric synthesis of linezolid thiazolidine-2-thione derivatives via CS2 mediated decarboxylation cyclization. Tetrahedron lett. 2020, 151847, . Qing Ji, Lihong Zhou, Hua Sui, Liu Yang, Xinnan Wu, Qing Song, Ru Jia, Ruixiao Li, Jian Sun, Ziyuan Wang, Ningning Liu, Yuanyuan Feng, Xiaoting Sun, Gang Cai, Yu Feng, Jianfeng Cai, Yihai Cao, Guoxiang Cai, yan wang, and Qi Li.* Primary tumors release ITGBL1-rich extracellular vesicles to promote distal metastatic tumor growth through fibroblast-niche formation. Nat. Commun. 2020, 11, 1211. Peng Sang,+ Yan Shi,+ Junhao Lu,+ Lihong Chen, Leixiang Yang, Wade Borcherds, Sami Abdulkadir, Qi Li,* Gary Daughdrill,* Jiandong Chen,* and Jianfeng Cai.* α-Helix-Mimicking Sulfono-γ-AApeptide Inhibitors for p53-MDM2/MDMX Protein–Protein Interactions. J. Med. Chem. 2020, 63, 3, 975-986. Mi Zhou,+ Mengmeng Zheng,+ and Jianfeng Cai.* Small molecules with membrane-active antibacterial activity. ACS. Appl. Mater. Inter. 2020, 12, 19, 21292-21299 Olapeju Bolarinwa, Chunpu Li, Nawal Khadka, Qi Li, Yan Wang, Jianjun Pan,* and Jianfeng Cai.* γ-AApeptides–based Small Molecule Ligands That Disaggregate Human Islet Amyloid Polypeptide. Sci. Rep., 2020, 10, 95. Sylvia Singh, Minghui Wang, Ruixuan Gao, Peng Teng, Timothy Odom, En Zhang, Hai Xu, and Jianfeng Cai.* Lipidated α/Sulfono-α-AA heterogeneous peptides as antimicrobial agents for MRSA. Bioorg. Med. Chem., 2020, 28, 115241. Lulu Wei, Minghui Wang, Ruixuan Gao, Rojin Fatirkhorani and Jianfeng Cai.* Antibacterial activity of lipo-α/sulfono-γ-AA hybrid peptides. Eur. J. Med. Chem., 2020, 186, 11901.