Research graph
References from Fragment-Based Covalent Targeting of Lysines at the Allosteric Latch Site of SHP2. Local targets link to admitted publications; unresolved targets remain external evidence.
A Comprehensive Review of SHP2 and Its Role in Cancer
10.1007/s13402-022-00698-1 · 2022 · External reference
Tyrosine Phosphatase PTPN11/SHP2 in Solid Tumors - Bull’s Eye for Targeted Therapy?
10.3389/fimmu.2024.1340726 · 2024 · External reference
Setting Sail: Maneuvering SHP2 Activity and Its Effects in Cancer
10.1016/bs.acr.2023.03.003 · 2023 · External reference
Allosteric Inhibition of SHP2 Phosphatase Inhibits Cancers Driven by Receptor Tyrosine Kinases
10.1038/nature18621 · 2016 · External reference
Strategies to Overcome Drug Resistance Using SHP2 Inhibitors
10.1016/j.apsb.2021.03.037 · 2021 · External reference
Allosteric SHP2 Inhibitors in Cancer: Targeting the Intersection of RAS, Resistance, and the Immune Microenvironment
10.1016/j.cbpa.2020.11.007 · 2021 · External reference
Crystallographic Landscape of SHP2 Provides Molecular Insights for SHP2 Targeted Drug Discovery
10.1002/med.21890 · 2022 · External reference
Advances in SHP2 Tunnel Allosteric Inhibitors and Bifunctional Molecules
10.1016/j.ejmech.2024.116579 · 2024 · External reference
Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2)
10.1021/acs.jmedchem.3c02118 · 2024 · External reference
Recent Advances in the Discovery of Protein Tyrosine Phosphatase SHP2 Inhibitors
10.1039/d1md00386k · 2022 · External reference
The Ascension of Targeted Covalent Inhibitors
10.1021/acs.jmedchem.1c02134 · 2022 · External reference
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: An Update
10.1021/acs.jmedchem.3c01825 · 2024 · External reference
Advanced Approaches of Developing Targeted Covalent Drugs
10.1039/d2md00216g · 2022 · External reference
Advancements, Challenges, and Future Frontiers in Covalent Inhibitors and Covalent Drugs: A Review
10.1016/j.ejmcr.2024.100217 · 2024 · External reference
Targeted Covalent Inhibitors for Novel Therapeutics
10.4155/fmc-2023-0243 · 2023 · External reference
Profiling Nuclear Cysteine Ligandability and Effects on Nuclear Localization Using Proximity Labeling-Coupled Chemoproteomics
10.1016/j.chembiol.2023.11.010 · 2024 · External reference
Allosteric Covalent Inhibitors of the STAT3 Transcription Factor from Virtual Screening
10.1021/acsmedchemlett.4c00622 · 2025 · External reference
An Intracellular Peptide Library Screening Platform Identifies Irreversible Covalent Transcription Factor Inhibitors
10.1002/advs.202416963 · 2025 · External reference
Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy
10.1021/acs.jmedchem.3c02403 · 2024 · External reference
Covalent Fragment Mapping of KRasG12C Revealed Novel Chemotypes with in Vivo Potency
10.1016/j.ejmech.2023.115212 · 2023 · External reference
Blocking C-Terminal Processing of KRAS4b via a Direct Covalent Attack on the CaaX-Box Cysteine
10.1073/pnas.2410766122 · 2025 · External reference
Discovery of Carbodiimide Warheads to Selectively and Covalently Target Aspartic Acid in KRASG12D
10.1021/jacs.5c03562 · 2025 · External reference
Discovering Uncharted Binding Pockets on E3 Ligases Leads to the Identification of FBW7 Allosteric Modulators
10.1002/advs.202506068 · 2025 · External reference
Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy
10.3389/fchem.2021.691093 · 2021 · External reference
Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications
10.1021/acschembio.8b01083 · 2019 · External reference
Drug Discovery Approaches to Target E3 Ligases
10.1002/cbic.202400656 · 2025 · External reference
Covalent Fragment Approaches Targeting Non-Cysteine Residues
10.1016/j.tips.2023.08.014 · 2023 · External reference
Design of Next-Generation Covalent Inhibitors: Targeting Residues beyond Cysteine
10.1016/bs.armc.2020.10.001 · 2020 · External reference
Advancing Covalent Ligand and Drug Discovery beyond Cysteine
10.1021/acs.chemrev.5c00001 · 2025 · External reference
The Expanding Repertoire of Covalent Warheads for Drug Discovery
10.1016/j.drudis.2023.103799 · 2023 · External reference
Covalent Inhibitors: To Infinity and Beyond
10.1021/acs.jmedchem.4c01308 · 2024 · External reference
A Proteome-Wide Atlas of Lysine-Reactive Chemistry
10.1038/s41557-021-00765-4 · 2021 · External reference
Mapping the SHP2 Allosteric Pocket With Target-Biased Covalent Fragments
10.1002/cbic.70310 · 2026 · External reference
An Electrophilic Warhead Library for Mapping the Reactivity and Accessibility of Tractable Cysteines in Protein Kinases
10.1016/j.ejmech.2020.112836 · 2020 · External reference
Assessment of Tractable Cysteines for Covalent Targeting by Screening Covalent Fragments
10.1002/cbic.202000700 · 2020 · External reference
Dual Allosteric Inhibition of SHP2 Phosphatase
10.1021/acschembio.7b00980 · 2018 · External reference
Design, Synthesis and Biological Evaluation of Novel Triazoloquinazolinone and Imidazoquinazolinone Derivatives as Allosteric Inhibitors of SHP2 Phosphatase
10.1080/14756366.2022.2078968 · 2022 · External reference
Design, Synthesis, and Biological Evaluation of Novel Triazoloquinazolinone Derivatives as SHP2 Protein Inhibitors
10.1080/14756366.2021.1986491 · 2021 · External reference
Crystal Structure, DFT Study, Hirshfeld Surface Analysis, Molecular Docking and Antitumor Activity of a Novel SHP2 Inhibitor
10.1016/j.molstruc.2023.137320 · 2024 · External reference
Electrophilic Warheads in Covalent Drug Discovery: An Overview
10.1080/17460441.2022.2034783 · 2022 · External reference
Global Profiling of Lysine Reactivity and Ligandability in the Human Proteome
10.1038/nchem.2826 · 2017 · External reference
Covalent Activation of the C-Type Lectin DC-SIGN
10.1002/anie.202520594 · 2025 · External reference
A Road Map for Prioritizing Warheads for Cysteine Targeting Covalent Inhibitors
10.1016/j.ejmech.2018.10.010 · 2018 · External reference
Profiling Sulfur(VI) Fluorides as Reactive Functionalities for Chemical Biology Tools and Expansion of the Ligandable Proteome
10.1021/acschembio.2c00633 · 2023 · External reference
Intrinsic Reactivity Profile of Electrophilic Moieties to Guide Covalent Drug Design:: N -α-Acetyl-l-Lysine as an Amine Nucleophile
10.1039/c6md00017g · 2016 · External reference
Very Fast Prediction and Rationalization of PKa Values for Protein-Ligand Complexes
10.1002/prot.22102 · 2008 · External reference
PROPKA3: Consistent Treatment of Internal and Surface Residues in Empirical p K a Predictions
10.1021/ct100578z · 2011 · External reference
Improved Treatment of Ligands and Coupling Effects in Empirical Calculation and Rationalization of pKa Values
10.1021/ct200133y · 2011 · External reference
Synthesis of Triazoloquinazolinone Based Compounds as Tubulin Polymerization Inhibitors and Vascular Disrupting Agents
10.1016/j.ejmech.2016.03.056 · 2016 · External reference
Cell-Active, Irreversible Covalent Inhibitors Targeting a Surface-Exposed Non-Catalytic Lysine on Aurora a Kinase by Using Squarate Chemistry
10.1002/ange.202510763 · 2025 · External reference
Demystifying Functional Parameters for Irreversible Enzyme Inhibitors
10.1021/acs.jmedchem.4c01721 · 2024 · External reference
Fitting of Kinact and KI Values from Endpoint Pre-Incubation IC50 Data
10.1021/acsmedchemlett.4c00054 · 2024 · External reference
Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies
10.1021/acs.biochem.0c00104 · 2020 · External reference
Unresolved reference
External reference
An Intracellular Peptide Library Screening Platform Identifies Irreversible Covalent Transcription Factor Inhibitors
10.1002/advs.202416963 · ExternalCitation · doi-reference
Discovering Uncharted Binding Pockets on E3 Ligases Leads to the Identification of FBW7 Allosteric Modulators
10.1002/advs.202506068 · ExternalCitation · doi-reference
Cell-Active, Irreversible Covalent Inhibitors Targeting a Surface-Exposed Non-Catalytic Lysine on Aurora a Kinase by Using Squarate Chemistry
10.1002/ange.202510763 · ExternalCitation · doi-reference
Covalent Activation of the C-Type Lectin DC-SIGN
10.1002/anie.202520594 · ExternalCitation · doi-reference
Assessment of Tractable Cysteines for Covalent Targeting by Screening Covalent Fragments
10.1002/cbic.202000700 · ExternalCitation · doi-reference
Drug Discovery Approaches to Target E3 Ligases
10.1002/cbic.202400656 · ExternalCitation · doi-reference
Mapping the SHP2 Allosteric Pocket With Target-Biased Covalent Fragments
10.1002/cbic.70310 · ExternalCitation · doi-reference
Crystallographic Landscape of SHP2 Provides Molecular Insights for SHP2 Targeted Drug Discovery
10.1002/med.21890 · ExternalCitation · doi-reference
Very Fast Prediction and Rationalization of PKa Values for Protein-Ligand Complexes
10.1002/prot.22102 · ExternalCitation · doi-reference
A Comprehensive Review of SHP2 and Its Role in Cancer
10.1007/s13402-022-00698-1 · ExternalCitation · doi-reference
Setting Sail: Maneuvering SHP2 Activity and Its Effects in Cancer
10.1016/bs.acr.2023.03.003 · ExternalCitation · doi-reference
Design of Next-Generation Covalent Inhibitors: Targeting Residues beyond Cysteine
10.1016/bs.armc.2020.10.001 · ExternalCitation · doi-reference
Strategies to Overcome Drug Resistance Using SHP2 Inhibitors
10.1016/j.apsb.2021.03.037 · ExternalCitation · doi-reference
Allosteric SHP2 Inhibitors in Cancer: Targeting the Intersection of RAS, Resistance, and the Immune Microenvironment
10.1016/j.cbpa.2020.11.007 · ExternalCitation · doi-reference
Profiling Nuclear Cysteine Ligandability and Effects on Nuclear Localization Using Proximity Labeling-Coupled Chemoproteomics
10.1016/j.chembiol.2023.11.010 · ExternalCitation · doi-reference
The Expanding Repertoire of Covalent Warheads for Drug Discovery
10.1016/j.drudis.2023.103799 · ExternalCitation · doi-reference
Advancements, Challenges, and Future Frontiers in Covalent Inhibitors and Covalent Drugs: A Review
10.1016/j.ejmcr.2024.100217 · ExternalCitation · doi-reference
Synthesis of Triazoloquinazolinone Based Compounds as Tubulin Polymerization Inhibitors and Vascular Disrupting Agents
10.1016/j.ejmech.2016.03.056 · ExternalCitation · doi-reference
A Road Map for Prioritizing Warheads for Cysteine Targeting Covalent Inhibitors
10.1016/j.ejmech.2018.10.010 · ExternalCitation · doi-reference
An Electrophilic Warhead Library for Mapping the Reactivity and Accessibility of Tractable Cysteines in Protein Kinases
10.1016/j.ejmech.2020.112836 · ExternalCitation · doi-reference
Covalent Fragment Mapping of KRasG12C Revealed Novel Chemotypes with in Vivo Potency
10.1016/j.ejmech.2023.115212 · ExternalCitation · doi-reference
Advances in SHP2 Tunnel Allosteric Inhibitors and Bifunctional Molecules
10.1016/j.ejmech.2024.116579 · ExternalCitation · doi-reference
Crystal Structure, DFT Study, Hirshfeld Surface Analysis, Molecular Docking and Antitumor Activity of a Novel SHP2 Inhibitor
10.1016/j.molstruc.2023.137320 · ExternalCitation · doi-reference
Covalent Fragment Approaches Targeting Non-Cysteine Residues
10.1016/j.tips.2023.08.014 · ExternalCitation · doi-reference
Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies
10.1021/acs.biochem.0c00104 · ExternalCitation · doi-reference
Advancing Covalent Ligand and Drug Discovery beyond Cysteine
10.1021/acs.chemrev.5c00001 · ExternalCitation · doi-reference
The Ascension of Targeted Covalent Inhibitors
10.1021/acs.jmedchem.1c02134 · ExternalCitation · doi-reference
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: An Update
10.1021/acs.jmedchem.3c01825 · ExternalCitation · doi-reference
Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2)
10.1021/acs.jmedchem.3c02118 · ExternalCitation · doi-reference
Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy
10.1021/acs.jmedchem.3c02403 · ExternalCitation · doi-reference
Covalent Inhibitors: To Infinity and Beyond
10.1021/acs.jmedchem.4c01308 · ExternalCitation · doi-reference
Demystifying Functional Parameters for Irreversible Enzyme Inhibitors
10.1021/acs.jmedchem.4c01721 · ExternalCitation · doi-reference
Profiling Sulfur(VI) Fluorides as Reactive Functionalities for Chemical Biology Tools and Expansion of the Ligandable Proteome
10.1021/acschembio.2c00633 · ExternalCitation · doi-reference
Dual Allosteric Inhibition of SHP2 Phosphatase
10.1021/acschembio.7b00980 · ExternalCitation · doi-reference
Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications
10.1021/acschembio.8b01083 · ExternalCitation · doi-reference
Fitting of Kinact and KI Values from Endpoint Pre-Incubation IC50 Data
10.1021/acsmedchemlett.4c00054 · ExternalCitation · doi-reference
Allosteric Covalent Inhibitors of the STAT3 Transcription Factor from Virtual Screening
10.1021/acsmedchemlett.4c00622 · ExternalCitation · doi-reference
PROPKA3: Consistent Treatment of Internal and Surface Residues in Empirical p K a Predictions
10.1021/ct100578z · ExternalCitation · doi-reference
Improved Treatment of Ligands and Coupling Effects in Empirical Calculation and Rationalization of pKa Values
10.1021/ct200133y · ExternalCitation · doi-reference
Discovery of Carbodiimide Warheads to Selectively and Covalently Target Aspartic Acid in KRASG12D
10.1021/jacs.5c03562 · ExternalCitation · doi-reference
Allosteric Inhibition of SHP2 Phosphatase Inhibits Cancers Driven by Receptor Tyrosine Kinases
10.1038/nature18621 · ExternalCitation · doi-reference
Global Profiling of Lysine Reactivity and Ligandability in the Human Proteome
10.1038/nchem.2826 · ExternalCitation · doi-reference
A Proteome-Wide Atlas of Lysine-Reactive Chemistry
10.1038/s41557-021-00765-4 · ExternalCitation · doi-reference
Intrinsic Reactivity Profile of Electrophilic Moieties to Guide Covalent Drug Design:: N -α-Acetyl-l-Lysine as an Amine Nucleophile
10.1039/c6md00017g · ExternalCitation · doi-reference
Recent Advances in the Discovery of Protein Tyrosine Phosphatase SHP2 Inhibitors
10.1039/d1md00386k · ExternalCitation · doi-reference
Advanced Approaches of Developing Targeted Covalent Drugs
10.1039/d2md00216g · ExternalCitation · doi-reference
Blocking C-Terminal Processing of KRAS4b via a Direct Covalent Attack on the CaaX-Box Cysteine
10.1073/pnas.2410766122 · ExternalCitation · doi-reference
Design, Synthesis, and Biological Evaluation of Novel Triazoloquinazolinone Derivatives as SHP2 Protein Inhibitors
10.1080/14756366.2021.1986491 · ExternalCitation · doi-reference
Design, Synthesis and Biological Evaluation of Novel Triazoloquinazolinone and Imidazoquinazolinone Derivatives as Allosteric Inhibitors of SHP2 Phosphatase
10.1080/14756366.2022.2078968 · ExternalCitation · doi-reference
Electrophilic Warheads in Covalent Drug Discovery: An Overview
10.1080/17460441.2022.2034783 · ExternalCitation · doi-reference
Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy
10.3389/fchem.2021.691093 · ExternalCitation · doi-reference
Tyrosine Phosphatase PTPN11/SHP2 in Solid Tumors - Bull’s Eye for Targeted Therapy?
10.3389/fimmu.2024.1340726 · ExternalCitation · doi-reference
Targeted Covalent Inhibitors for Novel Therapeutics
10.4155/fmc-2023-0243 · ExternalCitation · doi-reference
