Synthesis and Evaluation of Ubiquitin-Dioxetane Conjugate as a Chemiluminescent Probe for Monitoring Deubiquitinase Activity
Bioconjugate Chemistry, 2021, Accepted
The 20S as a stand-alone proteasome in cells can degrade the ubiquitin-tag
Nature Communications, 2021, Accepted
Insight on the Order of Regioselective Ultrafast Formation of Disulfide Bonds in (Antimicrobial) Peptides and Miniproteins
Angewandte Chemie International Edition, 2021, Accepted
Synthesis and Delivery of a Stable Phosphorylated Ubiquitin Probe to Study Ubiquitin Conjugation in Mitophagy
Chemical Communications, 2021, 57, 9438 - 9441
Chemical Synthesis of Ubiquitinated Proteins for Biochemical Studies
(WILEY-VCH), 2021, 383-410, ISBN: 978-3-527-34660-8
Total Chemical Synthesis of Proteins
(WILEY-VCH), 2021, ISBN: 978-3-527-34660-8
Development of fluorescence-based competitive assay enabled the discovery of dimeric cyclicpeptide modulators of ubiquitin chains
Angewandte Chemie International Edition, 2021, 60, 7018 –7023, Hot Paper
Harnessing the Power of Transition Metals in Solid Phase Peptide Synthesis and Key Steps in (Semi)Synthesis of Proteins
Chemical Society Reviews, 2021, 50, 2367 - 2387
Enhanced Live-Cell Delivery of Synthetic Proteins Assisted by Cell-Penetrating Peptides Fused to DABCYL
Angewandte Chemie International Edition, 2021, 60,7333 –7343 (Highlighted in Nature Chemistry, 2021, 13, 517–519).
In vivo modulation of ubiquitin chains by N-methylated non- proteinogenic cyclic peptides
RSC Chemical Biology, 2021, 2, 513-522
General Synthetic Strategy for Regioselective Ultrafast Formation of Disulfide Bonds in Peptides and Proteins
Nature Communications, 2021, 12:870
On-Demand Detachment of Succinimides on Cysteine to Facilitate (Semi) Synthesis of Challenging Proteins
Journal of American Chemical Society, 2020, 142, 19558−19569
Examining the role of phosphorylation of p19INK4d on its stability and ubiquitination using chemical protein synthesis
Chemical Science, 2020, 11, 5526 - 5531
Gold(I)-Mediated Decaging or Cleavage of Propargylated Peptide Bond in Aqueous Conditions for Protein Synthesis and Manipulation
Journal of American Chemical Society, 2020, 142, 8203-8210
Affinity Maturation of Macrocyclic Peptide Modulators of Lys48‐linked Diubiquitin by a Twofold Strategy
Chemistry - A European Journal, 2020, 26, 8022 –8027
Total Chemical Synthesis of ISGylated-Ubiquitin Hybrid Chain Assisted by Acetamidomethyl Derivatives with Dual Functions
Bioconjugate Chemistry, 2020, 31, 3, 889-894
Examining Several Strategies for the Chemical Synthesis of Phosphorylated Histone H3 Reveals the Effectiveness of the Convergent Approach
European Journal of Organic Chemistry, 2020, 21, 3128-3132 (selected as a very important paper)
The Journey for the Total Chemical Synthesis of a 53 kDa Protein
Accounts of Chemical Research, 2019, 52, 12, 3361-3371
Palladium Mediated Cleavage of Thiazolidine Backbone Modified Proteins in Live Cells
Angewandte Chemie International Edition ,2019, 58, 13540-13549
De novo macrocyclic peptides that specifically modulate Lys48-linked ubiquitin chains
Nature Chemistry, 2019, 11, 644–652
Mirroring Life’s Building Blocks
Cell Chemical Biology, 2019, 26, 5, 645 - 651
Chemical Biology: Powerful Synergy Between Two Cultures
Israel Journal of Chemistry, 2019, 59, 3-6
Palladium Mediated Direct Disulfide Bond Formation in Proteins Containing S‐Acetamidomethyl‐Cysteine under Aqueous Conditions
Angewandte Chemie International Edition, 2019, 58, 5729-5733
Semi-synthesis of ubiquitinated histone H2B with a native or non-hydrolyzable linkage
Methods in Enzymology, 2019, 618, 1-27
Diverse Fate of Ubiquitin Chain Moieties: The Proximal is Degraded with the Target and the Distal Protects it from Removal and Recycles
Proceedings of the National Academy of Sciences, 2019, 116, 16, 7805-7812
FACT and Ubp10 collaborate to modulate H2B deubiquitination and nucleosome dynamics
eLife, 2019, 8:e40988
A Halogen Substitution in Isoquinoline Scaffold Switches the selectivity of Inhibition between USP2 and USP7
ChemBioChem, 2019, 20, 282-286
Palladium Prompted On-Demand Cysteine Chemistry for the Synthesis of Challenging and Uniquely Modified Proteins
Nature Communications, 2018, 9:3154; Featured in Nature Communications Editors' Highlights
Palladium mediated deallylation in fully aqueous conditions for native chemical ligation at aspartic and glutamic acid sites
Organic & Biomolecular Chemistry, 2018, 16, 4061-4064
Activity-Based Probes Developed by Applying a Sequential Dehydroalanine Strategy on Expressed Proteins Reveal a Potential α-globin Modulating Deubiquitinase
Angewante Chemie, 2018, International Edition, 57, 5645-5649
Chemical Chromatin Ubiquitylation
Current Opinions in Chemical Biology, 2018, 45:18–26.
Total Chemical Synthesis of Ester-Linked Ubiquitinated Proteins Unravels their Behavior with Deubiquitinases
Chemical Science, 2018, 9, 1661-1665
Total Chemical Synthesis of Histones and their Analogues Assisted by Native Chemical Ligation and Palladium Complexes
Nature Protocols, 2017, 12(11):2293-2322.
Switching Futile para-Quinone to Efficient ROS Generator: Ubiquitin Specific Protease-2 Inhibition, Electrocatalysis and Quantification
ChemBioChem, 2017, 18,1683 –1687, Highlighted in Cover Page
Total Chemical Synthesis of Methylated Analogues of Histone 3 Revealed KDM4D as a Potential Regulator of H3K79me3
Bioorganic and Medicinal Chemistry, 2017, 25(18):4966-4970.
Palladium in the Chemical Synthesis and Modification of Proteins
Angewandte Chemie International Edition ,2017, International Edition, 56,10644 –10655.
Total Chemical Synthesis of SUMO-2-Lys63-linked Diubiquitin Hybrid Chains Assisted by Removable Solubilizing Tags
Chemical Science, 2017, 8, 4027-4034.
Ubiquitin Signaling: Chemistry Comes to the Rescue
Journal of American Chemical Society, 2017, 139, 4971−4986. (Highlighted in Spotlights on Recent JACS Publications).
Encyclopedia of Reagents for Organic Synthesis 2016, DOI: 10.1002/047084289X.rn00922.pub2.
Synthetic uncleavable ubiquitinated proteins dissect proteasome deubiquitination and degradation and highlight distinctive fate of tetraubiquitin (# these authors contributed equally)
Journal of American Chemical Society, 2016, 138 (49), pp 16004–16015.
Understanding and predicting the potency of ROS-based enzyme inhibitors, exemplified by naphthoquinones and ubiquitin specific protease-2
Chemical Science, 2016, 7, 7079-7086
Palladium Assisted Cleavage of Peptides and Proteins Containing a Backbone Thiazolidine Linkage
Chemistry - A European Journal, 2016, 22, 14851 - 14855 (hot paper).
Palladium-Assisted Removal of a Solubilizing Tag from a Cys Side Chain To Facilitate Peptide and Protein Synthesis
Organic Letters, 2016, 18, 3026–3029, ACS Editor Choice
Protein ubiquitination via Dehydroalanine: Development and Insights into the Diastereoselective 1,4-Addition Step
Organic & Biomolecular Chemistry, 2016, 14, 4817 - 4823
Efficient Palladium Assisted One-pot and Rapid Deprotection of Cysteine(Acetamidomethyl) Following Native Chemical Ligation and/or Desulfurization to Expedite Chemical Protein Synthesis
Angewandte Chemie International Edition ,2016, 55, 8108 - 8112
Palladium Mediated Rapid Deprotection of N-terminal Cysteine Under Native Chemical Ligation Conditions for the Efficient Preparation of Synthetically Challenging Proteins
Journal of American Chemical Society, 2016, 138 ,5069–5075.
Chemical and Semisynthetic Approaches to Study and Target Deubiquitinases
Chemical Society Reviews, 2016, 45, 4171 - 4198
Structural Basis for Histone H2B deubiquitination by SAGA DUB Module
Science, 2016, 351 725-728
Expanding the Chemical Toolbox for the Synthesis of Large and Uniquely Modified Proteins
Nature Chemistry, 2016, 8, 407–418
Total Chemical Synthesis of Phosphorylated Histone H2A at Tyr57 Reveals Insight into the Inhibition Mode of the SAGA Deubiquitinating Module
Angewandte Chemie International Edition ,2016, 55, 4972-6.
Chemical and Semisynthesis of Modified Histones
Journal of Peptide Science, 2016, 22: 252–259 (Festschrift for the journal on occasion of the 70th birthday of Stephen BH Kent) DOI: 10.1002/psc.2848
Pushing the Boundaries of Chemical Protein Synthesis: The Case of Ubiquitin Chains, Polyubiquitinated Peptides and Proteins
The Chemical Record, 2016, 16, 509–519
Chemical synthesis of ubiquitin chains
Current Protocols in Chemical Biology, 2015, 7, 229-2448
Rapid optimization of labeled ubiquitinated peptides for monitoring deubiquitinases activities
Organic and Biomolecular Chemistry, 2015,13, 8182-8186.
Synthesis of N-Hydroxy Isopeptide Containing Proteins
Organic Letters, 2015, 17 (14), pp 3438–3441
Convergent Versus Sequential Protein Synthesis: The Case of Ubiquitinated and Glycosylated H2B
Angewandte Chemie International Edition, 2015, 54, 12374–12378
KPC1-Mediated Ubiquitination and Proteasomal Processing of NF-κB1 p105 to p50 Restricts Tumor Growth
Cell, 2015, 161, 2, p333–347
Chemical Synthesis of Phosphorylated Ubiquitin and Diubiquitin Exposes Positional Sensitivities of E1-E2 Enzymes and Deubiquitinases
Chemistry - A European Journal, Volume 21, Issue 20, May 11, 2015, 7360–7364.
Harnessing the Oxidation Susceptibility of Deubiquitinases for Inhibition with Small Molecules
Angewandte Chemie International Edition, 2015, 54, 599-603
Angewandte Chemie International Edition, 2014, 53, 1738
Solid Phase Chemical Ligation Employing a Rink Amide Linker for the Synthesis of Histone H2B Protein
ChemComm, 2014, 50, 12534-7.
Rapid End-Group Modification of Polysaccharides for Biomaterial Applications in Regenerative Medicine
Macromolecular Rapid Communications 2014, 35, 20, 1754-1762.
Extended ubiquitin species are protein-based DUB inhibitors
Nature Chemical Biology, 2014, 10(8), 664-U212.
The U4/U6 recycling factor SART3 has histone chaperone activity and associates with USP15 to regulate H2B deubiquitination
Journal of Biological Chemistry, 2014, 289(13), 8916-30.
Non-Enzymatic Polyubiquitination od Expressed proteins
Journal of the American Chemical Society 2014, 136 (6),2665–2673. Highlighted 1) ACS Editor Choice; 2) Spotlights on Recent JACS Publications 3) ACS Chemical Biology.
Chemical protein synthesis
Journal of Peptide Science 2014, 20, 2, 63.
Dehydroalanine-Based Diubiquitin Activity Probes
Organic Letters, 2014, 16, 540–543.
Synthesis of tetra-ubiquitinated α-Synuclein reveals novel insights into the roles of ubiquitin chain in regulating pathophysiology
Proceeding National Academy of Science. USA, 2013, vol. 110 no.44, 17726–17731. Highlighted in 1) a commentary by Ivan Dikic et al in PNAS (Breaking the limits of artifical ubiquitination),PNAS, 2013, vol. 110 no.44, 17606–17607.2)News of the Week of C&EN. Issue: Vol. 91, #38, Sept. 23, 2013
Modifying the Vicinity of the Isopeptide Bond to Reveal Differential Behavior of Ubiquitin Chains with Interacting Proteins: Organic Chemistry Applied to Synthetic Proteins
Angewandte Chemie International Edition 2013, 52, 11149 –11153
One-pot total chemical synthesis of human alpha-synuclein
Chemical Communications, 2013,49,9254
Wolfgang Fischle*: Systematic identification of proteins binding to chromatin-embedded ubiquitylated H2B reveals recruitment of the SWI/SNF complex to regulate transcription
Cell Reports, 2013, 4, 601-608
Convergent Chemical Synthesis of Histone H2B Protein Enabled Site Specific Ubiquitination at Lys34
Angewandte Chemie International Edition 2013,52, 8059-8063. Selected by the editors as a Hot Paper
Chemistry and biology of peptides, proteins and beyond
Bioorganic and Medicinal Chemistry, 2013, 21, 3398-3399; (Editorial, Special BMC issue in honor of the 2013 Tetrahedron Young Investigator Award winner Professor Ashraf Brik).
Highly Efficient One-Pot Ligation and Desulfurization
Chemical Science, 2013, 4(6), 2496-2501.
Non-Enzymatic Synthesis of Ubiquitin Chains: Where Chemistry Makes a Difference
Bioorganic and Medicinal Chemistry, 2013, 21, 3411-3420; (Special BMC issue in honor of the 2013 Tetrahedron Young Investigator Award winner Professor Ashraf Brik).
Dissecting the Roles of the N- and C-flanking Residues of Acetyl-lysine Substrate for SIRT1 activity
ChemBioChem, 2013, 14, 577–581.
N-methylation of Isopeptide Bond as a Strategy to Resist Deubiquitinases
Angewandte Chemie International Edition 2012, 51(46), 11535-9.
Polymerization Behavior of a Bifunctional Ubiquitin Monomer as a Function of the Nucleophile Site and Folding Conditions
Journal of the American Chemical Society, 2012, 134(38),16085-16092
Chemistry and Biology of the Ubiquitin Signal (Invited Review)
Angewandte Chemie International Edition 2012, 51, 6840-6862.
The Size of the Proteasomal Substrate Determines whether its Degradation will be Mediated by Mono- or Polyubiquitylation
Molecular Cell, 2012, 48, 1-11. Highlighted in Nature Reviews Molecular Cell Biology 13, 602 (October 2012) DOI: 10.1038/nrm3445
Native Chemical Ligation at Glutamine
Organic Letters, 2012, 14, 1520-1523. Highlighted in the Peptides virtual issue that compiles the most noteworthy recent research in the field that were published in Org Lett, JOC and JACS; September 7, 2012, Volume 1, Issue 2
RNF20 and USP44 regulate embryonic stem cell differentiation by modulating H2B monoubiquitylation
Molecular Cell, 2012, 46, 662-673.
Chemical and Semisynthesis of Posttranslationally Modified Proteins
Organic & Biomolecular Chemistry, 2012, 10, 5684-5697
Targeting Deubiquitinases Enabled by Chemical Synthesis of Proteins
Journal of the American Chemical Society, 2012, 134, 3281-3289.
Chemical Synthesis of Ubiquitinated Peptides with Varying Lengths and Types of Ubiquitin Chains to Explore the Activity of Deubiquitinases
Angewandte Chemie International Edition 2012,51, 758–763.
Guest Editorial: Chemical Protein Synthesis
Israel Journal of Chemistry, 2011, 51, 852-853
Fighting Hepatitis C Virus with Peptide Nanotubes
Chemistry and Biology, 2011, 18, 1347-1348. (Invited Commentary)
δ-Mercaptolysine Assisted Ubiquitination
Israel Journal of Chemistry, 2011, 51, 900-907. (Special Issue on Protein Synthesis, Edited by Ashraf Brik, Philip E. Dawson, Stephen BH Kent)
Segmental Isotopic Labelling of Ubiquitin Chains to Unravel Monomer-Specific Molecular Behavior
Angewandte Chemie International Edition 2011, 50, 11210–11214
Self-Recognition Mechanism of MamA, a Magnetosome-Associated TPR-Containing Protein, Promotes Complex Assembly
Proceedings of the National Academy of Science, USA, 2011, 108, E480-E487
Total Synthesis of a 304 residue, K48-Linked Tetraubiquitin
Angewandte Chemie International Edition, 2011,50, 6137-6141;. Selected by the editors as a Hot Paper. See highlight on this paper in News of the Week of C&EN, May 30, 2011, Volume 89, number 22, p. 7
xploring the Self-Assembly of Glycopeptides Using Diphenylalanine Scaffold
Organic & Biomolecular Chemistry, 2011, 9, 5755-5761
Chemical Synthesis and Expression of the HIV-1 Rev Protein
ChemBioChem, 2011, 12, 1097-1104
Expeditious Chemical Synthesis of Ubiquitinated Peptides Employing Orthogonal Protection, Native Chemical Ligation
Bioconjugate Chemistry (ACS publication), 2011, 22, 137-143.
Towards elucidating the role of ubiquitination in the pathogenesis of Parkinson’s disease using semisynthetic ubiquitinated α-synuclein
Angewandte Chemie International Edition 2011, 50, 405.
Side-Chain Assisted Ligation: Scope and limitation
Journal of Peptide Science, 2011, 17, 252-255.
Total Chemical Synthesis of all di-Ubiqutin Chains, Angewandte Chemie Int. Ed. 2010,49, 9126-9131
This communication has been selected as a frontispiece for Angewandte Chemie International Edition. See highlights about this paper: 1) C&EN, Vol 88 # 41, October 11, 2010; 2) Carpe Diubiquitin, by L. Martin & R. T. Raines, Angewandte Chemie Int. Ed. 2010,49, 9042-9044;3) C&EN, December 20, 2010, issue: Chemical Year in Review 2010
Protein Synthesis Assisted by Native Chemical Ligation at Leucine
ChemBioChem, 2010, 11, 1232-1235
Accessing Posttranslationally Modified Proteins through Thiol Positioning
Journal of Peptide Science, 2010, 16, 524-529
Protecting Group Variations of δ-Mercaptolysine Useful in Chemical Ubiquitylation
Biopolymers, 2010, 94, 504-510.
New Strategies for Glycopeptides, Neoglycopeptides and Glycoproteins Synthesis, In Comprehensive Natural Products II Chemistry and Biology
Mander, L., Lui, H.-W., Eds.; Elsevier: Oxford, 2010; volume 6, pp.55–89.
N-Methylcysteine-Mediated Total Chemical Synthesis of Ubiquitin Thioester
Organic & Biomolecular Chemistry, 2010, 8, 2392-2396
Highly Efficient and Chemoselective Peptide Ubiquitylation
Angewandte Chemie International Edition, 2009, 48, 8090-8094; See highlight on this paper in C&EN, November 16, 2009, Volume 87.
Side-Chain Assisted Ligation in Protein Synthesis
Bioorganic & Medicinal Chemistry Letters, 2009, 19, 3870–3874.
Switch Peptide via Staudinger Reaction
Organic Letters, 2008, 11, 5243-5246.
Metathesis in Peptides and Peptidomimetics
Advanced Synthesis and Catalysis, 2008, 350, 1661-1675.
Peptide Ligation via Side-Chain Auxiliary
Chemical Communications, 2008, 10, 1229-1231.
AB2, an Azide-Alkyne Click Compound, is a Potent Protease Inhibitor of Multidrug-Resistant HIV-1
Journal of Medicinal Chemistry, 2008, 51, 6263-6267.
Sugar-Assisted Glycopeptide Ligation with Complex Oligosaccharides
Journal of The American Chemical Society, 2008, 130, 11945-11952
Extended Sugar-Assisted Glycopeptide Ligations
Development, Scope and Applications” Journal of The American Chemical Society, 2007, 129, 13527-13536
Sugar-Assisted Ligation in Glycoprotein Synthesis
Journal of the American Chemical Society, 2007, 129, 7690-7701.
Sugar-Assisted Ligation for the Synthesis of Glycopeptides
Chemistry-A European Journal, 2007, 13, 5670-5675.
Simon Ficht, Richard J. Payne, Ashraf Brik, Chi-Huey Wong
Chemistry-A European Journal, 2007, 13, 5670-5675.
Sugar Assisted ligation for the Synthesis of N-linked Glycopeptide with Broad Sequence Tolerance at the Ligation Junction
Journal of the American Chemical Society, 2006, 128, 15026-15033. See highlight about this paper in News & Views, Nature, 2007, 445, 31-33.
Strategies for the Preparation of Homogenous Glycoproteins,
Current Opinion in Chemical Biology, 2006, 10, 1-7.
Altered Gag-Pol Polyprotein Cleavage Specificity of FIV/HIV Mutant Proteases as Demonstrated in Cell-Based Expression System
Journal of Virology, 2006, 80, 7832-7843.
Sugar Assisted Glycopeptide Ligation
Journal of The American Chemical Society, 2006, 128, 5626-5627.
Microtiter Plate Based Chemistry and In Situ Screening: A Useful Approach for Rapid Inhibitors Discovery
Organic & Biomolecular Chemistry, 2006, 4, 1446-1457.
Epoxide Opening in Water for Rapid Inhibitor Discovery in Microtiter Plate and In situ screening
Bioorganic & Medicinal Chemistry, 2006, 14, 1058-1062
etrabutylammonium Fluoride-Mediated Rapid Alkylation Reaction in Microtiter Plates for Discovery of Enzyme Inhibitors In situ
ChemBiochem, 2005, 6, 2176-2180.
1,2,3 Triazole as a Peptide Bond Surrogate in the Rapid Synthesis of HIV Protease Inhibitors
ChemBiochem, 2005, 6, 1167-1169 (highlighted on the cover page)
Application to Combinatorial reaction in Microtiter plates for the Discovery of Potent Sulfotransferase Inhibitors In situ
Bioorganic & Medicinal Chemistry, 2005, 13, 4622-4626.
Catalytic Antibodies in Natural Product Synthesis” Catalytic Antibodies
Ehud Keinan, ed. (WILEY-VCH), 2005, 132-152
Small Molecules Targeting Severe Acute Respiratory Syndrome (SARS) Human Coronavirus
Proceedings of the National Academy of Science, USA, 2004, 101(27), 10012-10017.
Electrostatic interaction dominate the contribution of Arg39 in 44 Oxalocrotonate Tautomerase
Journal of the American Chemical Society, 2004, 126 (40), 12726-12727.
A model System for High-Throughput Screening of Novel Human Immunodeficiency Virus (HIV) Protease Inhibitors in Escherichia Coli
Antimicrobial Agents and Chemotherapy, 2004, 48(7), 2437-2447.
Rapid Discovery of Potent Sulfotransferase Inhibitors by Diversity-Oriented Reaction in Microplates Followed by in Situ Screening
ChemBioChem, 2004, 5, 811-819.
A Rapid Diversity-Oriented Synthesis and In Situ Screening of HIV Protease Inhibitors
ChemBioChem, 2003, 4, 1246-1248.
Design and Synthesis of Broad-Based Mono- and Bi-cyclic Inhibitors of FIV and HIV Proteases
Bioorganic & Medicinal Chemistry, 2003, 11, 2025-2040
Mechanism and Drug Discovery
Organic & Biomolecular Chemistry, 2003, 1, 5-14 (highlighted on the cover page),(Top 10 most downloaded OBC articles in 2006-2007 and 2009).
A Quick Diversity-Oriented Amide-Forming Reaction to Optimize p-subsite Residues of HIV Protease Inhibitors
Chemistry & Biology, 2002, 9, 891-896
Mutants of 4-Oxalocrotonate Tautomerase Catalyze the Decarboxylation of Oxaloacetate Through an Imine Mechanism
ChemBioChem, 2002, 3, 845-851, (highlighted on the cover page).
The Product of the Natural Reaction Catalyzed by 4-oxalocrotonate Tautomerase Becomes an Affinity Label of its Mutant
Bioorganic & Medicinal Chemistry, 2002,10, 3891-3897.
Protein Synthesis by Solid-Phase Chemical Ligation Using a Safety Catch Linker
Journal of Organic Chemistry, 2000, 65, 3829-3835
Studies Towards Total Synthesis of Borrelidin, Stereoselective Synthesis of the Polysubstituted Macrolidic Part
Tetrahedron Letters, 1997, 38, 6075-6078
Studies Towards Total Synthesis of Borrelidin, Regioselective Methylation of Bis-epoxides and Structure Determination
Tetrahedron Letters 1997, 38, 6079-6082.
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