Novel PROTACs for degradation of SHP2 protein

Protein tyrosine phosphatases: from genes, to function, to disease

Tonks, N. K. (2006) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2039 · Cited by 1,685 · see citing works

The ‘Shp'ing news: SH2 domain-containing tyrosine phosphatases in cell signaling

Neel, B. G., Gu, H., & Pao, L. (2003) · Trends in Biochemical Sciences · doi:10.1016/s0968-0004(03)00091-4 · Cited by 1,249 · see citing works

SHP-1 and SHP-2 Associate with Immunoreceptor Tyrosine-Based Switch Motif of Programmed Death 1 upon Primary Human T Cell Stimulation, but Only Receptor Ligation Prevents T Cell Activation

Chemnitz, J. M., Parry, R. V., Nichols, K. E., June, C. H., & Riley, J. L. (2004) · The Journal of Immunology · doi:10.4049/jimmunol.173.2.945 · Cited by 1,246 · see citing works

Programmed cell death 1 forms negative costimulatory microclusters that directly inhibit T cell receptor signaling by recruiting phosphatase SHP2

Yokosuka, T., Takamatsu, M., Kobayashi-Imanishi, W., Hashimoto-Tane, A., Azuma, M., & Saito, T. (2012) · Journal of Experimental Medicine · doi:10.1084/jem.20112741 · Cited by 1,161 · see citing works

Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

Chen, Y.-N. P., LaMarche, M. J., Chan, H. M., Fekkes, P., Garcia-Fortanet, J., Acker, M. G., Antonakos, B., Chen, C. H.-T., Chen, Z., Cooke, V. G., et al. (2016) · Nature · doi:10.1038/nature18621 · Cited by 925 · see citing works

Small‐Molecule PROTACS: New Approaches to Protein Degradation

Toure, M., & Crews, C. M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201507978 · Cited by 674 · see citing works

PROTACs: great opportunities for academia and industry

Sun, X., Gao, H., Yang, Y., He, M., Wu, Y., Song, Y.-G., Tong, Y., & Rao, Y. (2019) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-019-0101-6 · Cited by 651 · see citing works

Targeted protein degradation by PROTACs

Neklesa, T. K., Winkler, J. D., & Crews, C. M. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.02.027 · Cited by 599 · see citing works

RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers

Nichols, R. J., Haderk, F., Stahlhut, C., Schulze, C. J., Hemmati, G., Wildes, D., Tzitzilonis, C., Mordec, K., Marquez, A., Romero, J., et al. (2018) · Nature Cell Biology · doi:10.1038/s41556-018-0169-1 · Cited by 415 · see citing works

Docking and scoring with ICM: the benchmarking results and strategies for improvement

Neves, M., Totrov, M., & Abagyan, R. (2012) · Journal of Computer-Aided Molecular Design · doi:10.1007/s10822-012-9547-0 · Cited by 357 · see citing works

Protein tyrosine phosphatases in the JAK/STAT pathway

Xu, D. (2008) · Frontiers in bioscience · doi:10.2741/3051 · Cited by 309 · see citing works

PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery

Gu, S., Cui, D., Chen, X., Xiong, X., & Zhao, Y. (2018) · BioEssays · doi:10.1002/bies.201700247 · Cited by 231 · see citing works

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

Su, S., Yang, Z., Gao, H., Yang, H., Zhu, S., An, Z., Wang, J., Li, Q., Chandarlapaty, S., Deng, H., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00871 · Cited by 208 · see citing works

Characterization of phosphotyrosine binding motifs in the cytoplasmic domain of B and T lymphocyte attenuator required for association with protein tyrosine phosphatases SHP-1 and SHP-2

Gavrieli, M., Watanabe, N., Loftin, S. K., Murphy, T. L., & MURPHY, K. M. M. (2003) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2003.11.070 · Cited by 190 · see citing works

Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule

Zhao, Q., Lan, T., Su, S., & Rao, Y. (2018) · Chemical Communications · doi:10.1039/c8cc07813k · Cited by 185 · see citing works

Targeting SHP2 as a promising strategy for cancer immunotherapy

Liu, Q., Qu, J., Zhao, M., Xu, Q., & Sun, Y. (2019) · Pharmacological Research · doi:10.1016/j.phrs.2019.104595 · Cited by 177 · see citing works

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Wang, M., Lu, J., Wang, M., Yang, C.-Y., & Wang, S. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00471 · Cited by 172 · see citing works

Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment

Xie, J., Si, X., Gu, S., Wang, M., Shen, J. H., Li, H., Shen, J. H., Li, D., Fang, Y., Liu, C., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01520 · Cited by 113 · see citing works

Targeted protein knockdown using small molecule degraders

Raina, K., & Crews, C. M. (2017) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2017.05.016 · Cited by 111 · see citing works

6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors

Sarver, P., Acker, M., Bagdanoff, J. T., Chen, Z., Chen, Y.-N., Chan, H., Firestone, B., Fodor, M., Fortanet, J., Hao, H., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01726 · Cited by 87 · see citing works

PROTACs as Potential Therapeutic Agents for Cancer Drug Resistance

Sun, X., & Rao, Y. (2019) · Biochemistry · doi:10.1021/acs.biochem.9b00848 · Cited by 87 · see citing works

Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2

LaRochelle, J. R., Fodor, M., Ellegast, J. M., Liu, X., Vemulapalli, V., Mohseni, M., Stams, T., Buhrlage, S. J., Stegmaier, K., LaMarche, M. J., et al. (2017) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2017.10.025 · Cited by 51 · see citing works

Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2

Wu, X., Xu, G., Li, X., Xu, W., Li, Q., Liu, W., Kirby, K. A., Loh, M. L., Li, J., Sarafianos, S. G., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00513 · Cited by 48 · see citing works

SHP2 inhibitor specifically suppresses the stemness of KRAS-mutant non-small cell lung cancer cells

Jiang, L., Xu, W., Chen, Y., & Zhang, Y. (2019) · Artificial Cells Nanomedicine and Biotechnology · doi:10.1080/21691401.2019.1646748 · Cited by 26 · see citing works

Correction to “Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein”

Wang, M., Lu, J., Wang, M., Yang, C., & Wang, S. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c02108 · Cited by 9 · see citing works

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

Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · see citing works

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

He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00999-9 · Cited by 283 · see citing works

Developments of CRBN-based PROTACs as potential therapeutic agents

Wang, C., Zhang, Y., Wu, Y., & Xing, D. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113749 · Cited by 152 · see citing works

Double-edged roles of protein tyrosine phosphatase SHP2 in cancer and its inhibitors in clinical trials

Song, Y., Zhao, M., Zhang, H., & Yu, B. (2022) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2021.107966 · Cited by 125 · see citing works

A comprehensive review of SHP2 and its role in cancer

Asmamaw, M. D., Shi, X.-J., Zhang, L.-R., & Liu, H.-M. (2022) · Cellular Oncology · doi:10.1007/s13402-022-00698-1 · Cited by 119 · see citing works

PROTAC’ing oncoproteins: targeted protein degradation for cancer therapy

Kelm, J. M., Pandey, D. S., Malin, E., Kansou, H. W., Arora, S., Kumar, R., & Gavande, N. S. (2023) · Molecular Cancer · doi:10.1186/s12943-022-01707-5 · Cited by 115 · see citing works

Targeting protein phosphatases for the treatment of inflammation-related diseases: From signaling to therapy

Pan, J., Zhou, L., Zhang, C., Xu, Q., & Sun, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-01038-3 · Cited by 115 · see citing works

Targeting the undruggables—the power of protein degraders

Zhang, C., Liu, Y., Li, G., Yang, Z., Han, C., Sun, X., Sheng, C., Ding, K., & Rao, Y. (2024) · 中国科学通报：英文版 · doi:10.1016/j.scib.2024.03.056 · Cited by 108 · see citing works

SHP2: A Pleiotropic Target at the Interface of Cancer and Its Microenvironment

Sodir, N. M., Pathria, G., Adamkewicz, J. I., Kelley, E. H., Sudhamsu, J., Merchant, M. A., Chiarle, R., & Maddalo, D. (2023) · Cancer Discovery · doi:10.1158/2159-8290.cd-23-0383 · Cited by 103 · see citing works

Strategies Targeting Protein Tyrosine Phosphatase SHP2 for Cancer Therapy

Song, Y., Wang, S., Zhao, M., Yang, X., & Yu, B. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c02008 · Cited by 100 · see citing works

Computer-Aided Drug Discovery for Undruggable Targets

Sun, Q., Wang, H., Xie, J., Wang, L., Mu, J., Li, J., Ren, Y., & Lai, L. (2025) · Chemical Reviews · doi:10.1021/acs.chemrev.4c00969 · Cited by 69 · see citing works

Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC)

Chen, Y. X., Yuan, X., Tang, M., Shi, M., Yang, T., Liu, K., Deng, D., & Chen, L. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105508 · Cited by 52 · see citing works

PROTACs: Novel tools for improving immunotherapy in cancer

Li, S., Chen, T., Liu, J., Zhang, H., Li, J., Wang, Z. P., & Shang, G. (2023) · Cancer Letters · doi:10.1016/j.canlet.2023.216128 · Cited by 52 · see citing works

Application and challenges of nitrogen heterocycles in PROTAC linker

Li, Y., Qu, J., Jiang, L., Peng, X., Wu, K., Chen, M., Peng, Y., & Cao, X. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116520 · Cited by 45 · see citing works

Emerging Pharmacotherapeutic Strategies to Overcome Undruggable Proteins in Cancer

Lu, Y., Yang, Y., Zhu, G., Zeng, H., Fan, Y., Guo, F., Xu, D., Wang, B., Chen, D., & Ge, G. (2023) · International Journal of Biological Sciences · doi:10.7150/ijbs.83026 · Cited by 41 · see citing works

Targeted Protein Degradation (TPD) for Immunotherapy: Understanding Proteolysis Targeting Chimera-Driven Ubiquitin-Proteasome Interactions

Kamaraj, R., Ghosh, S., Das, S., Sen, S., Kumar, P. R., Majumdar, M., Dasgupta, R., Mukherjee, S., Das, S., Ghose, I., et al. (2024) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.4c00253 · Cited by 37 · see citing works

Crystallographic landscape of SHP2 provides molecular insights for SHP2 targeted drug discovery

Song, Y., Yang, X., Wang, S., Zhao, M., & Yu, B. (2022) · Medicinal Research Reviews · doi:10.1002/med.21890 · Cited by 37 · see citing works

Progress of small molecules for targeted protein degradation: PROTACs and other technologies

Zhao, H., Xin, M., & Zhang, S. (2023) · Drug Development Research · doi:10.1002/ddr.22026 · Cited by 31 · see citing works

Small-Molecule PROTACs for Cancer Immunotherapy

Liu, Z., Zhang, Y., Xiang, Y., & Kang, X. (2022) · Molecules · doi:10.3390/molecules27175439 · Cited by 29 · see citing works

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

Liang, X., Ren, H., Han, F., Liang, R., Zhao, J., & Liu, H. S. (2023) · Medicinal Research Reviews · doi:10.1002/med.21992 · Cited by 28 · see citing works

PROTAC delivery in tumor immunotherapy: Where are we and where are we going?

Li, Y., Wu, Y., Gao, S., Sun, T., & Jiang, C. (2024) · Journal of Controlled Release · doi:10.1016/j.jconrel.2024.11.076 · Cited by 27 · see citing works

Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers

Hyun, S., & Shin, D. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222212142 · Cited by 25 · see citing works

PROTAC: Novel degradable approach for different targets to treat breast cancer

Wang, Z., Che, S., & Yu, Z. (2024) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2024.106793 · Cited by 25 · see citing works

Advances in SHP2 tunnel allosteric inhibitors and bifunctional molecules

Guo, Z., Duan, Y., Sun, K., Zheng, T., Liu, J., Xu, S., & Xu, J. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116579 · Cited by 25 · see citing works

Developments of PROTACs technology in immune-related diseases

Wang, C., Zhang, Y., Deng, J., Liang, B., & Xing, D. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115127 · Cited by 23 · see citing works

The Peptide PROTAC Modality: A New Strategy for Drug Discovery

Zhu, Y., Dai, Y., & Tian, Y. (2025) · MedComm · doi:10.1002/mco2.70133 · Cited by 23 · see citing works

Targeting phosphatases: From molecule design to clinical trials

Guo, M., Li, Z., Gu, M., Gu, J., You, Q., & Wang, L. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116031 · Cited by 23 · see citing works

Binding Free Energy Calculation Based on the Fragment Molecular Orbital Method and Its Application in Designing Novel SHP-2 Allosteric Inhibitors

Yuan, Z., Chen, X., Fan, S., Chang, L., Chu, L., Zhang, Y., Wang, J., Li, S., Xie, J., Jian-guo, H., et al. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25010671 · Cited by 22 · see citing works

Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors

Tang, K., Zhao, M., Wu, Y.-H., Wu, Q., Wang, S., Dong, Y., Yu, B., Song, Y., & Liu, H.-M. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114106 · Cited by 20 · see citing works

Computational strategies for PROTAC drug discovery

Wu, J., Wang, W., & Leung, C. (2023) · Acta Materia Medica · doi:10.15212/amm-2022-0041 · Cited by 20 · see citing works

Application of PROTACs in target identification and validation

Liu, Y., Liang, J. Y., Zhu, R., Yang, Y., Wang, Y., Wei, W., Li, H., & Chen, L. (2024) · Acta Materia Medica · doi:10.15212/amm-2024-0010 · Cited by 20 · see citing works

Design, Synthesis, and Biological Evaluation of HDAC Degraders with CRBN E3 Ligase Ligands

Lu, Y., Sun, D., Xiao, D., Shao, Y.-Y., Su, M., Zhou, Y., Li, J. X., Zhu, S., & Lu, W. P. (2021) · Molecules · doi:10.3390/molecules26237241 · Cited by 20 · see citing works

Targeted protein degradation using chimeric human E2 ubiquitin-conjugating enzymes

Taylor, J. D., Barrett, N., Cuesta, S. M., Cassidy, K. B., Pachl, F., Dodgson, J., Patel, R. J., Eriksson, T. M., Riley, A., Burrell, M. R., et al. (2024) · Communications Biology · doi:10.1038/s42003-024-06803-4 · Cited by 19 · see citing works

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

Shang, Y., Fu, S., Hao, Q., Ying, H., Wang, J., & Shen, T. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2023.107092 · Cited by 17 · see citing works

Small-molecule Modulators Targeting SHP2 for Cancer Therapy

Chen, Y., Mi, D., & Li, Y. (2022) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520622666220921093052 · Cited by 16 · see citing works

Discovery of a SHP2 Degrader with In Vivo Anti-Tumor Activity

Miao, J., Bai, Y., Miao, Y., Qu, Z., Dong, J., Zhang, R., Aggarwal, D., Jassim, B. A., Nguyen, Q. D., & Zhang, Z. (2023) · Molecules · doi:10.3390/molecules28196947 · Cited by 16 · see citing works

Bivalent target-binding bioPROTACs induce potent degradation of oncogenic SHP2

Hoffman, M., Krum, D., & Wittrup, K. D. (2024) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2024.107616 · Cited by 16 · see citing works

Oxidative stress promotes fibrosis in systemic sclerosis through stabilization of a kinase-phosphatase complex

Zhang, R., Kumar, G. S., Hansen, U. J., Zoccheddu, M., Sacchetti, C., Holmes, Z. J., Lee, M. C., Beckmann, D., Wen, Y., Mikulski, Z., et al. (2022) · JCI Insight · doi:10.1172/jci.insight.155761 · Cited by 15 · see citing works

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

Zhao, X., Chen, Y., Su, H., & Zhang, L. (2023) · Interdisciplinary medicine · doi:10.1002/inmd.20230004 · Cited by 14 · see citing works

Discovery of TK-642 as a highly potent, selective, orally bioavailable pyrazolopyrazine-based allosteric SHP2 inhibitor

Tang, K., Wang, S., Feng, S., Yang, X., Guo, Y., Ren, X., Bai, L., Yu, B., Liu, H., & Song, Y. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.03.028 · Cited by 12 · see citing works

Ferroptosis triggers anti-tumor immunity via promoting chaperone-mediated autophagic degradation of SHP2

Zhu, J., Li, X., Chen, W., Zuo, Z., Gong, Q., Hu, J., Huang, K., Liu, W., Gu, Y., Xu, Q., et al. (2025) · Redox Biology · doi:10.1016/j.redox.2025.103796 · Cited by 12 · see citing works

Therapeutic efficacy of the novel SHP2 degrader SHP2-D26, alone or in combination, against lung cancer is associated with modulation of p70S6K/S6, Bim and Mcl-1

Deng, Y., Ma, G., Vallega, K. A., Wang, D., Wang, M., Wang, C., Wang, S., Ramalingam, S. S., & Sun, S. (2022) · Cancer Gene Therapy · doi:10.1038/s41417-022-00472-3 · Cited by 12 · see citing works

Discovery of small molecule degraders for modulating cell cycle

Wang, L., Yang, Z., Li, G., Liu, Y., Ai, C., & Rao, Y. (2023) · Frontiers of Medicine · doi:10.1007/s11684-023-1027-5 · Cited by 10 · see citing works

Self-Assembled Matrine-PROTAC Encapsulating Zinc(II) Phthalocyanine with GSH-Depletion-Enhanced ROS Generation for Cancer Therapy

Lai, S., Wang, B., Sun, K., Li, F., Liu, Q., Yu, X., Jiang, L., & Wang, L. (2024) · Molecules · doi:10.3390/molecules29081845 · Cited by 10 · see citing works

Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines

Hu, J., Yang, J., Zhou, R., Chen, K., Zhao, H., & Zhou, Y. (2025) · Biochemical Pharmacology · doi:10.1016/j.bcp.2025.117159 · Cited by 10 · see citing works

Proteolysis-Targeting Chimera Molecules Targeting SHP2

Yu, D., Zheng, M., Liu, Y., Chen, L., & Li, H. (2022) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0324 · Cited by 9 · see citing works

Drugging Protein Tyrosine Phosphatases through Targeted Protein Degradation

Miao, J., & Zhang, Z. (2024) · ChemMedChem · doi:10.1002/cmdc.202300669 · Cited by 8 · see citing works

Setting sail: Maneuvering SHP2 activity and its effects in cancer

Welsh, C. L., Allen, S., & Madan, L. K. (2023) · Advances in cancer research · doi:10.1016/bs.acr.2023.03.003 · Cited by 8 · see citing works

Discovery of SA-8 as a potent SHP2-AUTAC degrader in cancer therapy

Song, H., Zou, X., Liang, J., Huang, H. F., Liu, Y., Zhang, Y., Liu, Y., Chen, L., & Li, H. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117918 · Cited by 7 · see citing works

Role of Non-Receptor-Type Tyrosine Phosphatases in Brain-Related Diseases

He, Y., Nan, D., & Wang, H. (2023) · Molecular Neurobiology · doi:10.1007/s12035-023-03487-5 · Cited by 7 · see citing works

Therapeutic potential of targeting protein tyrosine phosphatases in liver diseases

Wang, A., Zhang, Y., Lv, X., & Liang, G. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.05.006 · Cited by 7 · see citing works

PD-L1/SHP2 dual PROTACs inhibit melanoma by enhancing T-cell killing activity

Liu, Y., Liang, J., Zheng, M., Song, H., Chen, L., & Li, H. (2024) · Chinese Chemical Letters · doi:10.1016/j.cclet.2024.110317 · Cited by 7 · see citing works

Phosphatase Dysregulation in Cancer: Signaling Pathways and Therapeutic Opportunities

Jama, M., Overduin, M., & Barakat, K. (2025) · MedComm – Oncology · doi:10.1002/mog2.70028 · Cited by 7 · see citing works

Diterpenoids from Euphorbia lathyris L.: a comprehensive review update

Wang, X., Xu, Y., Wang, Y.-L., Lin, F., Li, H., & Chen, L.-X. (2025) · Phytochemistry Reviews · doi:10.1007/s11101-025-10100-1 · Cited by 4 · see citing works

Self-assembled Nano-PROTACs: bridging chemical design and biological barriers in targeted protein degradation

Zhang, N., Liang, J.-X., Hu, B.-N., Wang, Y., An, H., & Wang, H. (2026) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2026.115861 · Cited by 5 · see citing works

A Novel Gain-of-Signal Assay to Detect Targeted Protein Degradation

Hoffman, M., Cheah, K. M., & Wittrup, K. D. (2024) · ACS Synthetic Biology · doi:10.1021/acssynbio.3c00447 · Cited by 5 · see citing works

Cross the Undruggable Barrier, the Development of SHP2 Inhibitors: From Catalytic Site Inhibitors to Allosteric Inhibitors

Guo, Y. L., Xu, Y., Dong, X., & Zhang, J. (2021) · ChemistrySelect · doi:10.1002/slct.202100186 · Cited by 5 · see citing works

Update on Structure and Function of SH2 Domains: Mechanisms and Emerging Targeting Strategies

Kasembeli, M. M., Rodas, J., & Tweardy, D. J. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26189060 · Cited by 4 · see citing works

PROTACs in targeted protein degradation: Advances in development and AI-enhanced drug discovery

Du, M., Liu, T., Wang, W., Fan, S., Tian, M., Du, Q., Wang, Z., Li, X., Liu, X., Xia, Q., et al. (2026) · European Journal of Medicinal Chemistry Reports · doi:10.1016/j.ejmcr.2026.100332 · Cited by 4 · see citing works

Design, Synthesis, and Anticancer Activity Evaluation of the New SHP2 Degraders

Zhao, J., Guo, X., Li, Z., Wang, Y., Hu, L., Liu, W., & Ding, C. (2025) · ChemistrySelect · doi:10.1002/slct.202405728 · Cited by 3 · see citing works

Flourishing innovation in KRAS targeting: Recent advances in medicinal chemistry strategies and future perspectives

Shen, T., Fei, W., Hu, Z., Pang, M., Ma, J., Zhou, T., & Shang, Y. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.109345 · Cited by 3 · see citing works

Recent advances in targeted degradation in the RAS pathway

Ge, Z., Fan, Z., He, W., Zhou, G., Zhou, Y., Zheng, M., & Zhang, S. (2025) · Future Medicinal Chemistry · doi:10.1080/17568919.2025.2476387 · Cited by 5 · see citing works

Structure-Guided Design of Pyrazolopyrimidinones as Highly Potent and Selective Allosteric SHP2 Inhibitors

Song, Y., Ren, X., Yang, X., Xiong, J., Wang, W., Tang, K., & Yu, B. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00524 · Cited by 2 · see citing works

A novel matrine derivative B10 exerts its anti-liver cancer activity in vitro and in vivo via targeting FGFR3/PI3K/AKT signaling pathway

Wang, X., Xie, Y., Hu, Z., Wang, S., Li, M., Wu, L., Jiang, J. R., & Wang, L. (2026) · Molecular Diversity · doi:10.1007/s11030-025-11460-8 · Cited by 2 · see citing works

SHP2-targeted cancer therapeutics: Structural insights, inhibitor development and emerging modalities

Zhang, Y., Zhu, C., Si, C., Lin, Y., Guo, Q., Zhou, H., & Yu, Z. (2026) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2026.118708 · Cited by 2 · see citing works

Design and Synthesis of S ‐Acetophenylhydrazones of 5‐Methyl‐1,3,4‐Thiadiazole‐2‐Thiol as SHP2 Inhibitory Agents

Mitra, R., Kumar, S., Chaudhuri, A., Majumdar, S., Krishnamurthy, S., Agrawal, A. K., & Ayyannan, S. R. (2025) · Chemistry & Biodiversity · doi:10.1002/cbdv.202402997 · Cited by 1 · see citing works

Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting

Zhang, M., Wu, S., Liu, M., Li, H., Wang, L., Duan, F., Han, R., Shan, C., Jiang, Z., Liao, J., et al. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117988 · Cited by 1 · see citing works

PROTACs in cancer immunotherapy: a minireview

Köckenberger, J., Cárdenas, S., T., C. E., Gutkind, J. S., & Ferguson, F. M. (2025) · Biochemical Society Transactions · doi:10.1042/bst20253065 · Cited by 2 · see citing works

Design, synthesis, and biological evaluation of death-associated protein kinase 1 PROTACs

Wu, X., Li, R., Tian, W., Yao, J., Chen, D., Lee, T. H., & Liu, Y. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.109044 · Cited by 1 · see citing works

Targeting SHP2 for Cancer Treatment: Advances and Prospects

Song, Y., & Yu, B. (2023) · Springer eBooks · doi:10.1007/978-3-030-80962-1_256-1 · Cited by 1 · see citing works

New Therapeutic Chemical Modalities: Compositions, Modes-of-action, and Drug Discovery

Valeur, E. (2023) · Royal Society of Chemistry eBooks · doi:10.1039/9781788018982-00911

Structural biology and computer-aided drug design

Singh, P., Hassan, S., Mehdi, M. M., Kumar, V. R., & Biswas, K. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-27461-9.00008-1

Targeting SHP2 for Cancer Treatment: Advances and Prospects

Song, Y., & Yu, B. (2025) · Springer eBooks · doi:10.1007/978-3-032-00771-1_256

PROTACS- targeted protein degradation as a path to precision cancer therapeutics

Gatley, H. R., Fisher, P. B., & Das, S. K. (2025) · Advances in cancer research · doi:10.1016/bs.acr.2025.08.001

Targeting Protein Tyrosine Phosphatases via PROteolysis-TArgeting Chimeras (PROTACs): Current Developments and Prospects

Maccari, R. (2025) · Molecules · doi:10.3390/molecules30224449

Discovery of myrsinane diterpenoids from Euphorbia monostyla with cytotoxic potential

Kokanov, A., Yang, H., Tang, D., Kokanov, A., Zhao, J., & Hajiakber, A. (2026) · Phytochemistry · doi:10.1016/j.phytochem.2026.115063

Linker attachment points: “finishing touch” in PROTAC design

jiang, Q., Shi, H.-S., Zhao, C.-S., Wang, Z.-Y., Yu, M.-M., Zhang, X.-Y., & Liu, C.-J. (2026) · RSC Medicinal Chemistry · doi:10.1039/d6md00346j

Protein degraders targeting JAK/STAT3 signaling pathway are emerging therapeutic modalities for human cancers

Feng, X., Li, N., Chen, X., Cao, X., Dai, J., Xiong, S., & Yuan, Z. (2026) · Biochemical Pharmacology · doi:10.1016/j.bcp.2026.118532

BindingDB Entry 50017101: Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors.

BindingDB (2023) · UC San Diego · doi:10.7270/q26977nn

BindingDB Entry 50018659: Developments of CRBN-based PROTACs as potential therapeutic agents.

BindingDB (2024) · UC San Diego · doi:10.7270/q27948wc

BindingDB Entry 50019825: Developments of PROTACs technology in immune-related diseases.

BindingDB (2024) · UC San Diego · doi:10.7270/q2cr5zrz

BindingDB Entry 50022023: Application and challenges of nitrogen heterocycles in PROTAC linker.

BindingDB (2025) · UC San Diego · doi:10.7270/q2kp86vh

BindingDB Entry 50022804: Advances in SHP2 tunnel allosteric inhibitors and bifunctional molecules.

BindingDB (2026) · UC San Diego · doi:10.7270/q2v98dw4

BindingDB Entry 50016243: Strategies Targeting Protein Tyrosine Phosphatase SHP2 for Cancer Therapy.

BindingDB (2023) · UC San Diego · doi:10.7270/q2x92g9p

Targeted Degradation of the Oncogenic Phosphatase SHP2

Vemulapalli, V., Donovan, K. A., Seegar, T. C. M., Rogers, J. M., Bae, M., Lumpkin, R. J., Cao, R., Henke, M. T., Ray, S. S., Fischer, E. S., et al. (2021) · Biochemistry · doi:10.1021/acs.biochem.1c00377 · Cited by 43 · see citing works

Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders

Yang, X., Wang, Z., Pei, Y., Song, N., Xu, L., Feng, B., Wang, H., Luo, X., Hu, X., Qiu, X., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113341 · Cited by 85 · see citing works

Discovery of a SHP2 Degrader with In Vivo Anti-Tumor Activity

Miao, J., Bai, Y., Miao, Y., Qu, Z., Dong, J., Zhang, R., Aggarwal, D., Jassim, B. A., Nguyen, Q. D., & Zhang, Z. (2023) · Molecules · doi:10.3390/molecules28196947 · Cited by 16 · see citing works

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Wang, M., Lu, J., Wang, M., Yang, C.-Y., & Wang, S. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00471 · Cited by 172 · see citing works

Medicinal chemistry strategies for the development of protein tyrosine phosphatase SHP2 inhibitors and PROTAC degraders

Tang, K., Jia, Y.-N., Yu, B., & Liu, H. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112657 · Cited by 47 · see citing works