Chunmao He

Site-Specific Tyrosine Sulfation of Triabin via Semi-Synthesis Enhances Thrombin Inhibition through Synergistic Multiple-Mode Interactions

Zhenbang Xiao, Zeyuan Mo, Lin L, Chunmao He

Herein, we report the semisynthesis of site-specifically sulfated triabin─a 142-amino-acid lipocalin protein─at Tyr124. Functional assays reveal that sulfation enhances anticoagulant activity by ∼5-fold, demonstrating that even rigid scaffolds can benefit from this modification. Modeling studies uncover a synergistic mechanism wherein the sulfate …

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Scaling covalent ligand discovery through dynamic combinatorial library-versus-proteome screening

Yuchen Huang, Lexuan Hou, Ruiping He, Lei Zhu et autres

Mass spectrometry-based chemical proteomics enables unbiased assessment of ligand potency and selectivity across the proteome. However, current approaches remain limited by the low throughput of single-compound screening and reliance on pre-synthesized libraries. Here we devise a mechanism-driven "library-versus-proteome" platform that couples dynamic …

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Editorial: Exploration of the role of heme proteins in biology with experimental and computational methods

Dragan M. Popović, Sergey A. Siletsky, Chunmao He, M. R. Gunner

Studying how these biomolecules function can help design more efficient drugs or inhibitors and develop more effective treatments for disorders related to the clinically relevant mutations and dysfunction of heme proteins (Zhai et al., 2023;Lee et al., 2024). Synthetic bioinspired heme proteins …

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Total chemical synthesis of the N-terminal domain of TIMP2

Yuanmei Sun, Yuqi Zhang, Chunmao He

The migration and invasion of tumor cells are major contributors to mortality in malignant tumors. Studies have shown that matrix metalloproteinase 14 (MMP14) plays a crucial role in promoting tumor cell metastasis. Its activity can be suppressed by tissue inhibitor of metalloproteinases …

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Engineering an artificial His-brace mimic in azurin for catalytic oxidative cleavage of polysaccharides

Jindi Luo, Chunmao He

The design and semi-synthesis of azurin-based artificial metalloenzymes incorporating a histidine brace-mimicking DPA ligand tailored for oxidative carbohydrate cleavage.

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Expedited Site-Selective Modification of Peptides and Proteins at N-Terminal Cysteine Facilitated by Imidazole

Peng George Wang, Junjie Liu, Yang Huang, Anjing Lu et autres

Site-selective modification of peptide and protein using commercially available or readily synthesized reagents remains a critical need in advancing the study and manipulation of biological processes. Herein, we present an imidazole-assisted strategy for the selective modification of N-terminal cysteine (NCys) residues in …

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3-Methylpyrazole-Mediated C-Terminal Protein Modification

Xinyue Zhang, Chunmao He

We present a mild, highly efficient, and selective method for the aminolysis of acyl pyrazole at protein C termini. The protocol demonstrates a broad substrate scope, operational simplicity, and aqueous-compatible conditions. Its successful application to site-specific C-terminal modification and dual functionalization underscores …

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Preparation of Peptide C-Terminal Salicylaldehyde Ester Surrogates via a Hydrazide-Based Oxidation and Phenolysis Strategy

Shaomin Lin, Chunmao He

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Scaling Covalent Ligand Discovery via Library-Versus-Proteome Screening

Yuchen Huang, Ruiping He, Lin Feng Zhu, C. Xu et autres

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Facile incorporation of non-canonical heme ligands in myoglobin through chemical protein synthesis

Kewei Yi, Peng Wang, Chunmao He

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Author response for "Azole reagents enabled ligation of peptide acyl pyrazoles for chemical protein synthesis"

Peisi Liao, Chunmao He

Recent advances in chemical protein synthesis: method developments and biological applications

Suwei Dong, Ji‐Shen Zheng, Yiming Li, Huan Wang et autres

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