Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC

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Catalytic in vivo protein knockdown by small-molecule PROTACs

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Acquired Resistance to KRAS ^G12C Inhibition in Cancer

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Targeting KRAS mutant cancers with a covalent G12C-specific inhibitor

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Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations

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Discovery of a Covalent Inhibitor of KRAS ^G12C (AMG 510) for the Treatment of Solid Tumors

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Ras history: The saga continues

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Identification of the Clinical Development Candidate <b>MRTX849</b> , a Covalent KRASG12C Inhibitor for the Treatment of Cancer

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Targeted Degradation of Oncogenic KRAS ^G12C by VHL-Recruiting PROTACs

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Docking Covalent Inhibitors: A Parameter Free Approach To Pose Prediction and Scoring

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Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

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KRAS as a Therapeutic Target

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Exploring Targeted Degradation Strategy for Oncogenic KRASG12C

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KRAS: From undruggable to a druggable Cancer Target

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KRAS Dimerization Impacts MEK Inhibitor Sensitivity and Oncogenic Activity of Mutant KRAS

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A Comparative Analysis of Individual RAS Mutations in Cancer Biology

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Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

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Efficient targeted degradation via reversible and irreversible covalent PROTACs

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PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

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Ubiquitination-mediated protein degradation and modification: an emerging theme in plant-microbe interactions

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Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta

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The role of reversible and irreversible covalent chemistry in targeted protein degradation

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Mechanisms of Resistance to KRASG12C-Targeted Therapy

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Targeting biomolecules with reversible covalent chemistry

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Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

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Design and synthesis of selective degraders of EGFRL858R/T790M mutant

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Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics

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Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

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Targeting KRAS mutated non-small cell lung cancer: A history of failures and a future of hope for a diverse entity

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Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4

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Structural basis of the atypical activation mechanism of KRASV14I

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PROTAC-mediated degradation of KRAS protein for anticancer therapeutics

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Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

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Chemistries of bifunctional PROTAC degraders

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PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

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Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

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Covalent Warheads Targeting Cysteine Residue: The Promising Approach in Drug Development

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A bibliometric analysis of PROTAC from 2001 to 2021

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Annual review of PROTAC degraders as anticancer agents in 2022

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Targeting the undruggables—the power of protein degraders

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Clinical considerations for the design of PROTACs in cancer

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PROTAC therapy as a new targeted therapy for lung cancer

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De Novo Design of an Androgen Receptor DNA Binding Domain‐Targeted peptide PROTAC for Prostate Cancer Therapy

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Advancing targeted protein degradation for metabolic diseases therapy

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Hydrophobic tag-based protein degradation: Development, opportunity and challenge

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Research progress on Sirtuins (SIRTs) family modulators

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PROTACs: A novel strategy for cancer drug discovery and development

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Applications of covalent chemistry in targeted protein degradation

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Targeting KRAS mutations: orchestrating cancer evolution and therapeutic challenges

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Annual review of KRAS inhibitors in 2022

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Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRAS ^G12D

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Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation

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Advances in Targeted Therapy Against Driver Mutations and Epigenetic Alterations in Non-Small Cell Lung Cancer

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PROTACS: A technology with a gold rush-like atmosphere

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Emerging Pharmacotherapeutic Strategies to Overcome Undruggable Proteins in Cancer

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Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation

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Design and synthesis of proteolysis-targeting chimeras (PROTACs) as degraders of glutathione peroxidase 4

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Covalent Proximity Inducers

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Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions

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Design, synthesis and biological evaluation of KRASG12C-PROTACs

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From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation

Wang, S., He, F., Tian, C., & Sun, A. (2024) · Pharmaceuticals · doi:10.3390/ph17010100 · Cited by 32 · see citing works

A covalent BTK ternary complex compatible with targeted protein degradation

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Unleashing the Power of Covalent Drugs for Protein Degradation

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TACkling Cancer by Targeting Selective Protein Degradation

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The new direction of drug development: Degradation of undruggable targets through targeting chimera technology

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Multiple Strategies to Develop Small Molecular KRAS Directly Bound Inhibitors

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Eliminating oncogenic RAS: back to the future at the drawing board

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Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy

Kirschner, T., Müller, M. P., & Rauh, D. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c02403 · Cited by 24 · see citing works

Evolution of direct RAS inhibitors: from undruggable target to clinical breakthroughs

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Exploiting E3 ligases for lung cancer therapy: The promise of DCAF-PROTACs

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Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR–ABL–Positive Leukemia

Luo, Z., Lin, C., Yu, C., Yuan, C., Wu, W., Xu, X., Sun, R., Jia, Y., Wang, Y., Shen, J., et al. (2024) · Cancer Research · doi:10.1158/0008-5472.can-24-1093 · Cited by 19 · see citing works

Targeting KRAS in pancreatic cancer: Emerging therapeutic strategies

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Progress in RAS‐targeted therapeutic strategies: From small molecule inhibitors to proteolysis targeting chimeras

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Multiple medicinal chemistry strategies of targeting KRAS: State-of-the art and future directions

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Targeted degradation of oncogenic KRASG12V triggers antitumor immunity in lung cancer models

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Selected Approaches to Disrupting Protein–Protein Interactions within the MAPK/RAS Pathway

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Discovery of a NCOA4 Degrader for Labile Iron-Dependent Ferroptosis Inhibition

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Development of PROTACS degrading KRAS and SOS1

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The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors

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FuncPhos-STR: An integrated deep neural network for functional phosphosite prediction based on AlphaFold protein structure and dynamics

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The complex journey of targeting RAS in oncology

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Targeted therapy based on ubiquitin-specific proteases, signalling pathways and E3 ligases in non-small-cell lung cancer

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The Core Autophagy Protein ATG5 Regulates KRAS Degradation via the Ubiquitin-Proteasome Pathway

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Identification of Suitable Target/E3 Ligase Pairs for PROTAC Development using a Rapamycin-induced Proximity Assay (RiPA)Preprint

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Rational design of VHL-recruiting KRASG12C proteolysis-targeting chimeras based on molecular dynamics simulation

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Krasg12d Selective Vhl-Protac with Sparing Kraswt and Other Kras MutantsPreprint

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Discovery of ZJK-366 as a potent and selective PROTAC degrader of KRASG12D protein for the treatment of cancer

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Targeted Degradation of Oncogenic KRAS ^G12C by VHL-Recruiting PROTACs

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Design, synthesis and biological evaluation of KRASG12C-PROTACs

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