I. Protein chemical synthesis and engineering

a) de novo peptide/protein synthesis
b) peptide/protein bioconjugation/modification/editing

II. Chemical biology of proteins with post-translational modification

Homogeneous proteins with site-specific glycosylation, phosphorylation, methylation, acetylation and other PTMs, whose generation is difficult via protein expression, can be readily obtained by protein chemical synthesis.

III. Tota synthesis and medicinal chemistry of natural products

We are interested in the total synthesis of bioactive natural products (i.e, cyclic peptides and glycans) and the study on their medicinal chemistry.

IV. Drug discovery and translation

Synthetic biologics, Antibiotics, Synthetic glycan-based antibacterial vaccines, Targeted radionuclide therapy drug, Antibody-drug conjugate, High throughput screening platforms and AI-assisted drug discovery platforms for protein-protein interactions.

V. New polymers for material sciences

New polymer chemistry: in-house clickable Dialdehyde-Amine Polymerization (cDAP);
New polymer materials: recyclable self-healing materials, biocompatible degradable materials, and elastic polymeric materials.

---

I. NEW Methods developed in our lab

1) Chemoselective peptide ligation for protein chemical synthesis
     a) Ser/Thr Ligation (STL) (Proc. Natl. Acad. Sci. , 2013)




     b) Cysteine/Penicillamine ligation (CPL) (Angew. Chem. Int. Ed., 2020)




     c) Superfast Desulfurization (Chem 2022)



     d) N,O-Benzylidene Acetal Dipeptides (NBDs) for difficult peptide synthesis (Angew. Chem. Int. Ed. 2023)





2) New OPA chemistry in peptide/protein science

     a) OPA-amine protein bioconjugation

3) Peptide late-stage modification & editing

     a) Clickable tryptophan modification (Sci. Adv. 2024)



     b) Photochemical Indole-to-Quinazoline Editing (J. Am. Chem. Soc. 2025)



     c) peptide cyclization via thioketalization with ketones (Org. Lett. 2024)

4) Synthetic carbohydrate chemistry

     a) Ring-Closing Glycosylation (RCG) (J. Org. Chem. 2014)

II. Total synthesis and medicinal chemistry of natural products

1）Total synthesis of daptomycin ( J. Am. Chem. Soc., 2013）


J. Am. Chem. Soc. 2013, 135, 6272
J. Med. Chem. 2020, 63, 3161
ACS Med. Chem. Lett. 2020, 11, 1442

2) Total synthesis of teixobactin (Nature Communications. , 2016)


Nature Commun. 2016, 7, 12394
Bioorg. Med. Chem. 2017, 17, 30578
Bioorg. Med. Chem. 2018, 26, 1062

3) Total synthesis of Antibiotics A54145 (Org. Lett. , 2019)



4) Total synthesis of Antibiotics CDA3a (Org. Lett. , 2020)



5) Total synthesis of Malacidin A (Angew. Chem. Int. Ed. , 2020)



6）Total synthesis of mannopeptimycin (J. Am. Chem. Soc., 2021）

III. Chemical glycobiology of bacterial glycans

1）Total Synthesis of Pseudomonas aeruginosa 1244 Pilin Glycan
( J. Am. Chem. Soc., 2017）



2) A Solution to Chemical Pseudaminylation via a Bimodal Glycosyl Donor for Highly Stereocontrolled α- and β- Glycosylation (Org. Lett. , 2019)





3) Bacterial Pse metabolic labeling (ACS. Chem. Bio., 2018)



3) Synthetic Pse-based antibacterial vaccine

a) ( Acs. Cent. Sci., 2021）



b) ( Acs. Cent. Sci., 2024）

IV. Chemical biology of proteins with PTMs

1）HMGA1a ( Cell. Chem. Biol., 2021）


2) Adiponectin glycosylation (J. Am. Chem. Soc. , 2021)