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PUBLICATIONS

Azapeptides with unique covalent warheads as SARS-CoV-2 main protease inhibitors

Azapeptides

Kaustav Khatua, Yugendar R. Alugubelli, Kai S. Yang, Veerabhadra R Vulupala, Lauren R. Blankenship, Demonta Coleman, Sandeep Atla, Sankar P. Chaki, Chia-Chuan D. Cho, Shivangi Sharma, Erol C. Vatansever, Yuying Ma, Ge Yu, Benjamin W. Newman, Shiqing Su and Wenshe R. Liu*, “Azapeptides with Unique Covalent Warheads as SARS-CoV-2 Main Protease Inhibitors”, Antiviral Research 225, 2024, 105874.

Leveraging a Phage-Encoded Noncanonical Amino Acid: A NovelPathway to Potent and Selective Epigenetic Reader ProteinInhibitors

Leveraging

Peng-Hsun Chase Chen, Xuejiao S. Guo, Hanyuan E. Zhang, Gopal K. Dubey, Zhi Z. Geng, Carol A. Fierke, Shiqing Xu, J. Trae Hampton and Wenshe R. Liu*, “Leveraging a Phage-Encoded Noncanonical Amino Acid: A Novel Pathway to Potent and Selective Epigenetic Reader Protein Inhibitors”, ACS Cent. Sci., 2024, 10, 782-792.

BRD4354 Is a Potent Covalent Inhibitor against the SARS-CoV-2 Main Protease

BRD4354

Yan J. Sheng, Syuan-Ting A. Kuo, Tingyuan Yang, Hanyuan E. Zhang, David H. Russell, Xin Yan, Shiqing Xu, Wenshe R. Liu and Carol A. Fierke*, “BRD4354 Is a Potent Covalent Inhibitor against the SARS-CoV-2 Main Protease”, Biochemistry, 2024, 63, 402-406.

Discovery of First-in-Class PROTAC Degraders of SARS-CoV‑2 MainProtease

Discovery

Yugendar R. Alugubelli, Jing Xiao, Kaustav Khatua, Sathish Kumar, Long Sun, Yuying Ma, Xinyu R. Ma, Veerabhadra R. Vulupala, Sandeep Atla, Lauren R. Blankenship, Demonta Coleman, Xuping Xie, Benjamin W. Newman, Wenshe R. Liu and Shiqing Xu*, “Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease”, J. Med. Chem., 2024, 67, 6495-6507.

2023

An amber-encoding helper phage for more efficient phage display of noncanonical amino acids

Amber

J. Trae Hampton, Chia-Chuan D. Cho, Demonta D. Coleman, Zhi Z. Geng, Peng-Hsun C. Chen, Gopal K. Dubey, Lauralee D. Sylvain, Shiqing Xu and Wenshe R. Liu*, “An Amber-encoding Helper Phage for More Efficient Phage Display of Noncanonical Amino Acids”, Nucleic Acids Research, 2023, Vol. 51, No. 13, 6566-6577.

2023

A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease

Systematic

Zhi Z. Geng, Sandeep Atla, Namir Shaabani, Veerabhadra R. Vulupala, Kai S. Yang, Yugendar R. Alugubelli, Kaustav Khatua, Peng-Hsun Chen, Jing Xiao, Lauren R. Blankenship, Xinyu R. Ma, Erol C. Vantansever, Chia-Chuan D. Cho, Yuying Ma, Robert Allen, Henry Ji, Shiqing Xu and Wenshe R. Liu*, “A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease”, J. Med. Chem. 2023, 66, 3, 449-455.

A Novel Y-Shaped, S–O–N–O–S-Bridged Cross-Link between Three Residues C22, C44, and K61 Is Frequently Observed in the SARS-CoV-2 Main Protease

Novel

Kai S. Yang, Lauren R. Blankenship, Syuan-Ting Alex Kuo, Yan J. Sheng, Pringwei Li, Carol A. Fierke, David H. Russell, Xin Yan, Shiqing Xu* and Wenshe R. Liu*, “A Novel Y-Shaped, S-O-N-O-S-Bridged Crosslink between Three Residues C22, C44, and K61 Is a Redox Switch of the SARS-CoV-2 Main Protease”, ACS Chem. Biol 2023, 18, 3, 449-455.

Novel Regioselective Approach to Cyclize Phage-Displayed Peptides in Combination with Epitope-Directed Selection to Identify a Potent Neutralizing Macrocyclic Peptide for SARS-CoV-2

Novel

J. Trae Hampton, Tyler J. Lalonde, Jeffery M. Tharp, Yadagiri Kurra, Yugendar R. Alugubelli, Christopher M. Roundy, Gabriel L. Hamer, Shiqing Xu and W. R. Liu*, “Novel Regioselective Approach to Cyclize Phage-Displayed Peptides in Combination with Epitope-Directed Selection to Identify a Potent Neutralizing Macrocylic Peptide for SARS-CoV-2”, ACS Chem. Biol., 2022, 17, 2911-2922.

2022

Phage-assisted, active site-directed ligand evolution of apotent and selective histone deacetylase 8 inhibitor

pro4512-fig-0001-

Jared S. Morse, Yan J. Sheng, J. Trae Hampton, Lauralee D. Sylvain, Sukant Das, Yugendar R. Alugubelli, Peng-Hsun Chase Chen, Kai S. Yang, Shiqing Xu, Carol A. Fierke and W. R. Liu*, “Phage-assisted, Active Site-Directed Ligand Evolution of a Potent and Selective Histone Deacetylase 8 Inhibitor.”, Protein Science, 2022, 31:e4512.

MPI8 is Potent against SARS-CoV-2 by Inhibiting Dually and Selectively the SARS-CoV-2 Main Protease and the Host Cathepsin L**

cmdc202100456-toc-0001-m

Xinyu R. Ma, Yugendar R. Alugubelli, Yuyin Ma, Erol C. Vatansever, Danielle A. Scott, Yuchen Qiao, Ge Yu, Shiqing Xu*, and W. R. Liu*, “MPI8 is Potent Against SARS-CoV-2 by Inhibiting Dually and Selectively the SARS-CoV-2 Main Protease and the Host Cathepsin L”, Angew. Chem. 2022, 134, , 192-204.

2022

Titelbild: A Reversible Chemogenetic Switch for Chimeric Antigen Receptor T Cells (Angew. Chem. 10/2022)

ange202201860-toc-0001-m

Wenyue Cao, Zhi Zachary Geng, Na Wang, Quan Pan, Shaodong Guo, Shiqing Xu, Jianfeng Zhou* and W. R. Liu*, “A Reversible Chemogenetic Switch for Chimeric Antigen Receptor T Cell”, Angew. Chem. 2022, 134, , 192-204.

A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals

Eur J Med Chem_2022_Yugendar

Yugendar R. Alugubelli, Zhi ZacharyGeng, Kai S. Yang, Namir Shaabani, Kaustav Khatua, Xinyu R. Ma, Erol C. Vatansever, Chia-Chuan Cho, Yuying Ma, Jing Xiao, Lauren R. Blankenship, Ge Yu, Banumathi Sankaran, Pingwei Li, Robert Allen, Henry Ji, Shiqing Xu and W. R. Liu*, “A Systematic Exploration of Boceprevir-based Main Protease Inhibitors as SARS-CoV-2 Antivirals.”, Eur. J. Med. Chem., 2022, 240,114596.

Protein Synthesis via Activated Cysteine-Directed Protein Ligation

Fig1_Mothods Mol Bio_GY

Ge Yu, Yuchen Qiao, Lauren R Blankenship and W. R. Liu*, “Protein Synthesis Via Activated Cysteine-Directed Protein Ligation”, Methods Mol Biol., 2022, 2530;159-167.

Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir

J Med Chem_2022_K Yang

Kai S. Yang, Sunshine Z. Leeuwon, Shiqing Xu and Wenshe R. Liu*, “Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir”, J. Med. Chem., 2022, 65, 13, 8686-8698.

A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals

Eur J Med Chem_2022

Yuying Ma, Kai S. Yang, Zhi Zachary Geng, Yugendar R. Alugubelli, Namir Shaabani, Erol C. Vatansever, Xinyu R. Ma, Chia-Chuan Cho, Kaustav Khatua, Jin Xiao, Lauren R. Blankenship, Ge Yu, Banumathi Sankaran, Pingwei Li, Robert Allen, Henry Ji, Shiqing Su and W. R. Liu*, “A Multi-pronged Evaluation of Aldehyde-based Tripeptidyl Main Protease Inhibitors as SARS-CoV-2 Antivirals”, Eur. J. Med. Chem., 2022, 240,114570.

Taf2 mediates DNA binding of Taf14

Nat Commun_2022

Brianna J. Klein, Jordan T. Feigerle, Jibo Zhang, Christopher C. Ebmeier, Lixin Fan, Rohit K. Singh, Wesley W. Wang, Lauren R. Schmitt, Thomas Lee, Kirk C. Hansen, Wenshe R. Liu, Yun-Xing Wang, Brian D. Strahl, P. Anthony Weil, and Tatiana G. Kutateladze*, “Taf2 Mediates DNA Binding of Taf14”, Nat. Commun. 2022, 13(1), 3177.

Resveratrol Binds Nuclear Receptor 4A1 (NR4A1) and Acts as an NR4A1 Antagonist in Lung Cancer Cells

mol pharmacal_22

Lei Zhang, Greg Martin, Jumaravel Mohankumar, Joshua Trae Hampton, Wenshe R. Liu and Stephen Safe*, “Reseratrol Binds Nuclear Receptor 4A1 (NR4A1) and Acts as an NR4A1 Antagonist in Lung Cancer Cells”,Mol. Pharmacol., 2022, 102(2), 80-91. doi: 10.1124/molpharm.121.000481.

Accurate Mass Identification of an Interfering Water Adduct and Strategies in Development and Validation of an LC-MS/MS Method for Quantification of MPI8, a Potent SARS-CoV-2 Main Protease Inhibitor, in Rat Plasma in Pharmacokinetic Studies

pharmaceuticals-15-00676-g001_2022

Yang Wang, Huan Xie, Yugendar R. Alugubelli, Yuying Ma, Shiqing Xu, Jing Ma, Wenshe R. Liu and Dong Liang*, “Accurate Mass Identification of an Interfering Water Adduct and Strategies in Development and Validation of al LC-MS/MS Method for Quantification of MPI8, a Potent SARS-CoV-2 Main Protease Inhibitor, in Rat Plasma in Pharmacokinetic Studies”, Pharmaceuticals. 2022, 15(6), 676. doi: 10.3390/ph15060676.

An Enhanced Hybrid Screening Approach to Identify Potent Inhibitors for the SARS-CoV-2 Main Protease From the NCI Compound Library

fchem-10-816576-g0x1

Shuhua G. Li, Kai S. Yang, Lauren R. Blankenship, Chia-Chuan D. Cho, Shiqing Xu, Hongbin Wang and W. R. Liu*, “An Enhanced Hybrid Screening Approac ot Identify Potent Inhibitors for the SARS-CoV-2 Main Protease From the NCI Compound Library”, Front. Chem., 2022, 10,816575.

A Designed, Highly Efficient Pyrrolysyl-tRNA Synthetase Mutant Binds o-Chlorophenylalanine Using Two Halogen Bonds

1-s2.0-S0022283622001085-ga1_lrg

Erol C. Vatansever, Kai S. Yang, Zhi Zachary Geng, Yuchen Qiao, Pingwei Li, Shiqing Xu and W. R. Liu*, “A Designed, Highly Efficient Pyrrolysyl-tRNA Synthetase Mutant Binds o-Chlorophenylalanine Using Two Halogen Bonds”, J. Mol Biol, 2022, 167534.

The N-Terminal Carbamate is Key to High Cellular and Antiviral Potency for Boceprevir-Based SARS-CoV-2 Main Protease Inhibitors

Yugendar R. Alugubelli, Zhi Zachary Geng, Kai S. Yang, Namir Shaabani, Kaustav Khatua, Xinyu R. Ma, Erol C. Vatansever, Chia-Chuan Cho, Yuying Ma, Lauren Blankenship, Ge Yu, Banumathi Sankaran, Pingwei Li, Robert Allen, Henry Ji, Shiqing Xu and W. R. Liu*, “The N-Terminal Carbamate is Key to High Celluar and Antiviral Potency for Boceprevir-Based SARS-CoV-2 Main Protease Inhibitors”, bioRxiv 2022.

The P3 O-Tert-Butyl-Threonine is Key to High Cellular and Antiviral Potency for Aldehyde-Based SARS-CoV-2 Main Protease Inhibitors

Yuying Ma, Kai S. Yang, Zhi Zachary Geng, Yugendar R. Alugubelli, Namir Shaabani, Erol C. Vatansever, Xinyu R. Ma, Chia-Chuan Cho, Kaustave Khatua, Lauren Blankenship, Ge Yu, Banumathi Sankaran, Pingwei Li, Robert Allen, Henry Ji, Shiqing Xu and W. R. Liu*, “The P3 O-Tert-Butyl-Threonine is Key to High Celluar and Antiviral Potency for Aldehyde-Based SARS-CoV-2 Main Protease Inhibitors”, bioRxiv. 2022.

The Pyrrolysyl-tRNA Synthetase Activity can be Improved by a P188 Mutation that Stabilizes the Full-Length Enzyme

1-s2.0-S0022283622000171-ga1_CCC22

Chia-Chuan Cho, Lauren R. Blankenship, Xinyu Ma, Shiqing Xu and W. R. Liu*, “The Pyrrolysyl-tRNA Synthetase Activity can be Improved by a P188 Mutation that Stabilizes the Full-Length Enzyme”, J. Mol Biol, 2022, 434, 167453.

Drug Repurposing for the SARS-CoV-2 Papain-Like Protease

cmdc202100455-toc-0001-m_chemMedChem_CCC22

Chia-Chuan Cho, Shuhua G. Li, Tyler J. Lalonde, Kai S. Yang, Ge Yu, Yuchen Qiao, Shiqing Xu and W. R. Liu*, “Drug Repurposing for the SARS-CoV-2 Papain-Like Protease”, ChemMedChem. 2022, 17, e202100455.

Evaluation of SARS-CoV‑2 Main Protease Inhibitors Using a Novel Cell-Based Assay

a_images_large_oc1c00910_0007

Wenyue Cao, Chia-Chuan Dean Cho, Zhi Zachary Geng, Namir Shaabani, Xinyu R. Ma, Erol C. Vtansever, Yugendar r. Alugubelli, Yuying Ma, Sankar P. Chaki, William H. Ellenburgm Kai S. Yang, Yuchen Qiao, Robert Allen, Benjamin W. Neuman, Henry Ji, Shiqing Xu and W. R. Liu*, “Evaluation of SARS-CoV-2 Main Protease Inhibitors Using a Novel Cell-Based Assay”, ACS Cent Sci. 2022, 8, 2, 192-204.

Repurposing Halicin as Potent Covalent Inhibitor for the SARS-CoV-2 Main Protease

Repurposing Halicin as Potent Covalent Inhibitor for the SARS-CoV-2 Main Protease

K. S. Yang, Syuan-Ting Alex Kuo, Lauren R. Blankenshp, Zhi Zachary Geng, Shuhua G. Li, David H. Russell, Xin Yan, Shiqing Xu and W. R. Liu*, “Repurposing Halicin as Potent Covalent Inhibitor for the SARS-CoV-2 Main Protease”, Cur. Res. in Chem. Bio., 2022, 2, 100025.

2021

The Construction of a Genetically Encoded, Phage-Displayed Cyclic-Peptide Library

The Construction of a Genetically Encoded, Phage-Displayed Cyclic-Peptide Library

P-H C. Chen and W. R. Liu*, “The Construction of a Genetically Encoded, Phage-Displayed Cyclic-Peptide Library”, Chapter of Peptide Conjugation, Eds. W. M. Hussein, R. J. Stephenson & I. Toth, Springer Science+Business Media, LLC., 219-230.

2021

Discovery of Selective Small-Molecule Inhibitors for the ENL YEATS Domain

Discovery of Selective Small-Molecule Inhibitors for the ENL YEATS Domain

Xy R. Ma, L Xu, S. Xu, B. J. Klein, Hk Wang, S. Das, K. Li, K. S. Yang, S. Sohail, A. Chapman, T. G. Kutateladze, Xb. Shi and W. R. Liu*, “Discovery of Selective Small-Molecule Inhibitors for the ENL YEATS Domain”, J. Med. Chem. 2021, 64, 10997-11013.

Site-Specific Conversion of Cysteine in a Protein to Dehydroalanine Using 2-Nitro-5-thiocyanatobenzoic Acid

Site-Specific Conversion of Cysteine in a Protein to Dehydroalanine Using 2-Nitro-5-thiocy

Y. Qiao, G. Yu, S. Z. Leeuwon and W. R. Liu*, “Site-Specific Conversion of Cysteine in a Protein to Dehydroalanine Using 2-Nitro-5-thiocyanatobenzoic Acid”, Molecules, 2021, 2619.

Bepridil is potent against SARS-CoV-2 in vitro

Bepridil is potent against SARS-CoV-2 in vitro

E. C. Vatansever, K. S. Yang, K. C. Kratch, A. Drelich, C.-C. Cho, K. R. Kempaiah, J. C. Hsu, D. M. Mellott, S. Xu, C.-T. K. Tseng*, and Liu W.R.*, “Bepridil is Potent Against SARS-CoV-2 In Vitro”, Proc. Natl. Acad. Sci. U. S. A., 2021, 118(10): e2012201118.

2020

A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors

A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors

K. S. Yang, X. R. Ma, Y. Ma, Y. R. Alugubell, D. A. Scott, E. C. Vatansever, A. K. Drelich, B. Sankaran, Z. Z. Geng, L. R. Blankenship, H. E. Ward, Y. J. Sheng, J. C. Hsu, K. C. Kratch, B. Zhao, H. S. Hayatshsshi, J. Liu, P. Li, C. A. Fierke*, C.-T. K. Tseng*, S. Xu* and W. R. Liu*, “A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors”, ChemMedChem2021,DOI: 10.1002/cmdc.202000924 (VIP paper): 10.1002/cmdc.202000924 (VIP paper).

2020

Site Specific Lysine Acetylation of Histones for Nucleosome Reconstitution Using Genetic Code Expansion in Escherichia coli

C. M. Rowlett and W. R. Liu*, “Site Specific Lysine Acetylation of Histones for Nucleosome Reconstitution Using Genetic Code Expansion in Escherichia coli”, J. Vis. Exp. 2020, DOI: 10.3791/62113.

A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors

An Optimal “Click” Formulation Strategy for Antibody-Drug Conjugate Synthesis

E. C. Vatansever, J. Kang, A. Tuley, E. S. Ward E.S.* and W. R. Liu*, “An Optimal “Click” Formulation Strategy for Antibody-Drug Conjugate Synthesis”, Bioorg. Med. Chem. 2020, 28(24): 115808.

The Molecular Basis of Tight Nuclear Techering and Inactivation of cGAS

The Molecular Basis of Tight Nuclear Techering and Inactivation of cGAS

Baoyu Zhao, Pengbiao Xu, Chesley M. Rowlett, Tao Jing, Omkar Shinde, Yuanjiu Lei, a. Phillip West, Wenshe Ray Liu* & Pingwei Li*, “The Molecular Basis of Tight Nuclear Techering and Inactivation of cGAS”, Nature, 2020https://doi.org/10.1038/s41586-020-2749-z.

A Speedy Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors

Kai_Figure_gourpwebsite_publication

K. S. Yang, X. R. M, Y. Ma Y, Y. R. Alugubelli, D. A. Scott, E. C. Vatansever, A. K. Drelich, B. Sankaran, Z. Z. Geng, L. R. Blankenship, H. E. Ward, Y. J. Shen, J. C. Hsu, K. C. Kratch, B. Zhao, H. S. Hayatshsshi, J. Liu, P. Li, C. A. Fierke, C.-T. K. Tseng, S. Xu and W. R. Liu*, “A Speedy Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors”, BioRxiv, 2020http://doi.org/10.1101/2020.07.28.223784.

Bepridil is Potent Against SARS-CoV-2 In Vitro

Bepridil is Potent Against SARS-CoV-2 In Vitroo

E. C. Vatansever, K. S. Yang, K. C. Kratch, A. Drelich, C.-C. Cho, D. M. Mellott, S. Xu, C.-T. K. Tseng, and W. R. Liu*, “Bepridil is Potent Against SARS-CoV-2 In Vitro”, BioRxiv, 2020http://doi.org/10.1101/2020.05.23.112235

Expressed Protein Ligation without Intein

Expressed Protein Ligation without Intein

Y. Qiao, G. Yu, X. A. Wang, K. C. Kratch, S. Z. Leeuwon, W. W. Wang, J. S. Morse, and W. R. Liu*, “Expressed Protein Ligation without Intein”, J. Am. Chem. Soc. 2020, 142: 7047-7054.

Stepwise Assembly of Turn-on Fluorescence Sensors in Multicomponent Metal–Organic Frameworks for in Vitro Cyanide Detection

Stepwise Assembly of “Turn-on” Fluorescent Sensors in Multicomponent Metal-Organic Framewo

J. Li, S. Yuan, J. S. Qin, J. Pang, P. Zhang, Y. Zhang, Y. Huang, H. F. Drake, W. R. Liu, and H. C. Zhou*, “Stepwise Assembly of “Turn-on” Fluorescent Sensors in Multicomponent Metal-Organic Frameworks for in vitro Cyanide Detection”, Angew. Chem. Int. Ed., 2020,59, 9319-9323. DOI: 10.1002/anie.202000702.

An amber obligate active site-directed ligand evolution technique for phage display

An amber obligate active site-directed ligand

J. M. Tharp, J. T. Hampton, C. A. Reed, A. Ehnbom, P. C. Chen, J. S. Morse, Y. Kurra, L. M. Perez, S. Xu, W. R. Liu "An Amber Obligate Active Site-Directed Ligand Evolution Technique for Phage Display". Nat Commun. 2020, 11(1):1392.

Learning from the Past: Possible Urgent Prevention and Treatment Options for Severe Acute Respiratory Infections Caused by 2019-nCoV

Learning from the Past Possible Urgent Prevention

J. S. Morse, T. Lalonde, S Xu and W. R. Liu*, “Learning from the Past: Possible Urgent Prevention and Treatment Options for Severe Acute Respiratory Infections Caused by 2019-nCoV”, ChemBioChem, 2020, 21(5):730-738 (VIP paper).

2019

Histone H3K23-specific acetylation by MORF is coupled to H3K14 acylation

Nat Commun. 2019_s41467-019-12551-5

B. J. Klein, S. M. Jang, C. Lachance, W. Mi, J. Lyu, S. Sakuraba, K. Krajewski, W. W. Wang,  S. Sidoli, J. Liu, Y. Zhang, X. Wang, B. M. Warfield, A. J. Kueh, A. K. Voss, T. Thomas, B. A. Garcia, W. R. Liu, B. D. Strahl, H. Kono, W. Li, X. ShiX, J. Côté, T. G. Kutateladze."Histone H3K23-specific acetylation by MORF is coupled to H3K14 acylation". Nat Commun. 2019 Oct 17;10(1):4724. doi: 10.1038/s41467-019-12551-5. PubMed PMID: 31624313; PubMed Central PMCID: PMC6797804.

2019

A Genetically Encoded, Phage-Displayed Cyclic-Peptide Library

cyclic peptide-Angewandte

XS. Wang, P. C. Chen, J. T. Hampton, J. M. Tharp, C. A. Reed, S. K. Das, D. S. Wang,H. S. Hayatshahi, Y. Shen, J. Liu and W. R. Liu. "A Genetically Encoded, Phage-Displayed Cyclic-Peptide  Library". Angew Chem Int Ed Engl. 2019 Oct 28;58(44):15904-15909. doi: 10.1002/anie.201908713. Epub 2019 Sep 9. Review. PubMed PMID: 31398275; PubMed Central PMCID: PMC6803038.

Covalent Inhibition in Drug Discovery

CMC_Covalent inhibition

A. K. Ghosh, I. Samanta, A. Mondal, W. R. Liu. “Covalent Inhibition in Drug Discovery”. ChemMedChem. 2019 May 6;14(9):889-906. doi: 10.1002/cmdc.201900107. Epub 2019 Mar 26. Review. PubMed PMID: 30816012; PubMed Central PMCID: PMC6816337.

A Click Chemistry Approach Reveals the Chromatin-Dependent Histone H3K36 Deacylase Nature of SIRT7

ja-2018-12083q_0010

W. W. Wang, M. Angulo-Ibanez, J. Lyu, Y. Kurra, Z. Tong, B. Wu, L. Zhang, V. Sharma, J. Zhou, H. Lin, Y. Q Gao, W. Li, K. F. Chua and W. R. Liu. "A Click Chemistry Approach Reveals the Chromatin-Dependent Histone H3K36 Deacylase Nature of SIRT7". J Am Chem Soc. 2019 Feb 13;141(6):2462-2473. doi: 10.1021/jacs.8b12083. Epub 2019 Feb 4. PubMed PMID: 30653310; PubMed Central PMCID: PMC6812484.

Estrogen Improves Insulin Sensitivity and Suppresses Gluconeogenesis via the Transcription Factor Foxo1

Diabetes_Fig-1

H. Yan, W. Yang, F. Zhou, X. Li, Q. Pan, Z. Shen, G. Han, A. Newell-Fugate, Y. Tian, R. Majeti, W. Liu, Y. Xu, C. Wu, K. Allred, C. Allred, Y. Sun and S. Guo. "Estrogen Improves Insulin Sensitivity and Suppresses Gluconeogenesis via the Transcription Factor Foxo1". Diabetes. 2019 Feb;68(2):291-304. doi: 10.2337/db18-0638. Epub 2018 Nov 28. PubMed PMID: 30487265; PubMed Central PMCID: PMC6341301.

2018

Structural insights into the π-π-π stacking mechanism and DNA-binding activity of the YEATS domain

Nat Commun. 2018_s41467-018-07072-6

B. J. Klein, K. R. Vann, F. H. Andrews, W. W. Wang, J. Zhang, Y.i Zhang, A. A. Beloglazkina, W. Mi, Y. Li, H. Li, X. Shi, A. G. Kutaeladze, B. Strahl, W. R. Liu and T. G. Kutateladze. "Structural Insights into the π-π-π Stacking Mechanism and DNA-binding Activity of the YEATS Domain", Nat Commun. 2018, Nov. 1; 9(1): 4574. doi:10.1038/s41467-018-07072-6. PubMed PMID: 30385749; PubMed Central PMCID: PMC6212594.

2018

Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome

1-s2.0-S0092867418305269-fx1_lrg

B. T. Weinert, T. Narita, S. Satpathy, B, Srinivasan, B. K. Hansen, C. Schölz, W. B. Hamilton, B. E. Zucconi, W. W. Wang, W. R. Liu, J. M. Brickman, E. A. Kesicki, A. Lai, K. D. Bromberg, P. A. Cole, C. Choudhary. "Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome". Cell. 2018 Jun 28;174(1):231-244.e12. doi:
10.1016/j.cell.2018.04.033. Epub 2018 May 24. PubMed PMID: 29804834; PubMed Central PMCID: PMC6078418. 

Incorporation of Nonproteinogenic Amino Acids in Class I and II Lantibiotics

cb-2017-01024k_0008

N. Kakkar, J. G. Perez, W. R. Liu, M. C. Jewett, W. A. van der Donk. "Incorporation of Nonproteinogenic Amino Acids in Class I and II Lantibiotics". ACS Chem Biol. 2018 Apr 20;13(4):951-957. doi: 10.1021/acschembio.7b01024. Epub 2018 Feb 21. PubMed PMID: 29439566; PubMed Central PMCID: PMC5910287.

Using Amber and Ochre Nonsense Codons to Code Two Different Noncanonical Amino Acids in One Protein Gene

J. M. Tharp, W. R. Liu. "Using Amber and Ochre Nonsense Codons to Code Two Different Noncanonical Amino Acids in One Protein Gene". Methods Mol Biol. 2018;1728:147-154. doi: 10.1007/978-1-4939-7574-7_9. PubMed PMID: 29404996.10.1016/j.cell.2018.04.033. Epub 2018 May 24. PubMed PMID: 29804834; PubMed Central PMCID: PMC6078418. 

A Lipid Transfer Protein Signaling Axis Exerts Dual Control of Cell-Cycle and Membrane Trafficking Systems

1-s2.0-S1534580717310432-fx1

J. Huan, C. J. Mousley, L. Dacquay, N. Maitra, G. Drin, C. He, ND Ridgway, A. Tripathi, M. Kennedy, BK Kennedy, WS Liu, K. Baetz, M. Polymenis, V. A. Bankaitis. "A Lipid
Transfer Protein Signaling Axis Exerts Dual Control of Cell-Cycle and Membrane Trafficking Systems", Dev Cell. 2018 Feb 5; 44(3), 378-391.e5. doi: 10.1016/j.devcel.2017.12.026. Epub 2018 Jan 27. PubMed PMID: 29396115; PubMed Central PMCID: PMC6444186.

2017

Synthetases pick up the PACE

nchembio.2516-F1

Jeffery M. Tharp and Wenshe R. Liu*. "Genetic Code Expansion: Synthetases Pick Up the PACE", Nat Chem Biol., 2017, 13(12), 1205-1206. doi:10.1039/nchembio.2516. 

2017

Evolving the N-Terminal Domain of Pyrrolysyl-tRNA Synthetase for Improved Incorporation of Noncanonical Amino Acids

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Vangmayee Sharma, Yu Zeng, W. Wesley Wang, Yuchen Qiao, Yadagiri Kurra and Wenshe R. Liu*. "Evolving the N-Terminal Domain of Pyrrolysyl-tRNA Synthetase for Improved Incorporation of Noncanonical Amino Acids", ChemBioChem., 2017, 18, 1-6. doi:10.1002/cbic.201700268Transfer Protein Signaling Axis Exerts Dual Control of Cell-Cycle and Membrane Trafficking Systems", Dev Cell. 2018 Feb 5; 44(3), 378-391.e5. doi: 10.1016/j.devcel.2017.12.026. Epub 2018 Jan 27. PubMed PMID: 29396115; PubMed Central PMCID: PMC6444186.

Structure, function, and applications

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Jeffery M. Tharp, Andreas Ehnbom and Wenshe R. Liu*. "Structure, Function, and Applications", RNA Biol., 2017 Aug 24:1-12.doi:10.1080/15476286.2017.1356561

Proteins with Site-Specific Lysine Methylation

Chem Eur J_10.1002-chem

Zhipeng A. Wang and Wenshe R. Liu*. "Proteins with Site-Specific Lysine Methylation", Chem. Eur. J., 10.1002/chem.201701655.

A strategy for dual inhibition of the proteasome and fatty acid synthase with belactosin C-orlistat hybrids

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Mingzhao Zhu, Wayne D. Harshbarger, Omar Robles, Joanna Krysiak, Kenneth G. Hull, Sung Wook Chok, Robyn D. Richardson, Yanyan Yang, Andres Garcia, Lindsey Spiegelman, Bianca Ramirez, Christopher T. Wilson, Ju Anne Yau, James T. Moore, Caitlen B. Walker, James C. Sacchettini, Wenshe R. Liu, Stephan A. Sieber, Jeffrey W. Smith and Daniel Romo*. "A Strategy for Dual Inhibition of the Proteasome and Fatty Acid Synthase with Belactosin C-orlistat Hybrids", Bioorg. Med. Chem., 2017, 25, 2901-2916.

Genetically Encoded 2‑Aryl-5-carboxytetrazoles for Site-Selective Protein Photo-Cross-Linking

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ulin Tian, Marco Paolo Jacinto, Yu Zeng, Zhipeng Yu, Jun Qu, Wenshe R. Liu and Qing Lin*, and Wenshe R. Liu*. "Genetically Encoded 2-Aryl-5-carboxytetrazoles for Site-Selective Protein Photo-Cross-Linking", J. Am. Chem. Soc., 2017, 139, 6078-6081.

A Versatile Approach for Site-Specific Lysine Acylation in Proteins

angew chem ed 2017_56_1643

Zhipeng A. Wang, Yadagir Kurra, Xin Wang, Yu Zeng, Yan-Jiun Lee, Vangmayee Sharma, Hening Lin, Susie Y. Dai*, and Wenshe R. Liu*. "A Versatile Approach for Site-Specific Lysine Acylation in Proteins", Angew. Chem. Int. Ed., 2017, 56, 1643-1647.

A Genetically Encoded Allysine for the Synthesis of Proteins with Site-Specific Lysine Dimethylation

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Zhipeng A. Wang, Yu Zeng, Yadagir Kurra, Xin Wang, Jeffrey M. Tharp, Erol C. Vatansever, Willie W. Hsu, Susie Dai, Xinqiang Fang,* and Wenshe R. Liu*. "A Genetically Encoded Allysine for the Synthesis of Proteins with Site-specific Lysine Dimethylation", Angew. Chem. Int. Ed., 2017, 56, 212-216.

2016

Probing the Catalytic Charge-Relay System in Alanine Racemase with Genetically Encoded Histidine Mimetics

ACS Chem Biol 2016_11_3305

Vangmayee Sharma, Yane-Shih Wang, and Wenshe R. Liu, "Probing the Catalytic Charge-Relay System in Alanine Racemase with Genetically Encoded Histidine Mimetics”, ACS Chem Biol. 2016, 11, 3305-3309.

2016

Genetically encoded fluorophenylalanines enable insights into the recognition of lysine trimethylation by an epigenetic reader

Chem Commun_2016_52_12606

Yan-Jiun Lee, M. J. Schmidt, Jeffery M. Tharp, Annemarie Weber, Amber L. Koenig, Hong Zheng, Jianmin Gao, Marcey L. Waters, Daniel Summerer,* and Wenshe R. Liu* "Genetically Encoded Fluorophenylalanines Enable Insights into the Recognition of Lysine Trimethylation by an Epigenetic Reader" Chem. Commun., 2016, 52, 12606-12609.

A Chemical Biology Approach to Reveal Sirt6-targeted Histone H3 Sites in Nucleosomes

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Wang, Wesley Wei; Zeng, Yu; Wu, Bo; Deiters, Alexander and Liu, Wenshe*, "A Chemical Biology Approach to Reveal Sirt6-targeted Histone H3 Sites in Nucleosomes", ACS Chem. Biol., 2016, 11, 1973-1981.

Sirtuins 1 and 2 Are Universal Histone Deacetylases

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Hsu, Willie W.; Wu, Bo and Liu, Wenshe R.*, "Sirtuins 1 and 2 Are Universal Histone Deacetylases", ACS Chem. Biol., 2016, 11, 792-799.

The “π-Clamp” Offers a New Strategy for Site-Selective Protein Modification

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Tharp, Jeffery M. and Liu, Wenshe R.*, "The 'π-Clamp' Offers a Novel Strategy for Site-selective Protein Modification", ChemBioChem, 2016, 17, 883-885.

Phospha-Michael Addition as a New Click Reaction for Protein Functionalization

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Lee, Yan-Jiun; Kurra, Yadagiri and Liu, Wenshe R.*, "Phospha-Michael Addition as a New Click Reaction for Protein Functionalization", ChemBioChem, 2016, 17, 456-461.

2015

Fluorinated Aromatic Amino Acids Distinguish Cation-π Interactions from Membrane Insertion*

He, Tao; Gershenson, Anne; Eyles, Stephen J.; Lee, Yan-Jiun; Liu, Wenshe R.; Wang, Jiangyun; Gao, Jianmin; and Roberts, Mary F.*, "Fluorinated Aromatic Amino Acids Distinguish Cation-π Interactions from Membran Insertion", J. Biol. Chem, 2015, 290, 19334-19342.

2015

Facile Removal of Leader Peptides from Lanthipeptides by Incorporation of a Hydroxy Acid

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Bindman, Noah A; Boeica, Silvia C.; Liu, Wenshe R.; van der Donk, Wilfred A.*, "Facile Removal of Leader Peptides from Lanthipeptides by Incorporation of a Hydroxy Acid", J. Am. Chem. Soc., 2015, 137, 6975-6978.

Improving the bioactivity of rHirudin with boronophenylalanine site-specific modification

Xin, X; Liu, W. R; Sun, L.*, "Improving the bioactivity of rHirudin with boronophenylalanine site-specific modification", Mol. Med. Rep., 2015, 11, 3774-3779.

A click chemistry approach to site-specific immobilization of a small laccase enables efficient direct electron transfer in a biocathode

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Guan, Dongli; Kurra, Y; Liu, W. R.; Chen, Zhilei*, "A click chemistry approach to site-specific immobilization of a small laccase enables efficient direct electron transfer in a biocathode", Chem. Commun., 2015, 51, 2522-2525.

Expanding the chemical diversity of lasso peptide MccJ25 with genetically encoded noncanonical amino acids

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Piscotta, Frank J.; Tharp, Jeffery M.; Liu, W. R.; Link, A. James*, "Expanding the chemical diversity of lasso peptide MccJ25 with genetically encoded noncanonical amino acids", Chem. Commun., 2015, 51, 409-412.

Wenshe Liu's Bibliography

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