Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition

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PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors

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Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐x L Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches

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HDAC3 and HDAC8 PROTAC dual degrader reveals roles of histone acetylation in gene regulation

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Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment

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Targeted degradation of specific TEAD paralogs by small molecule degraders

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MDM2-BCL-XL PROTACs enable degradation of BCL-XL and stabilization of p53

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B‐cell lymphoma‐2 family proteins in the crosshairs: Small molecule inhibitors and activators for cancer therapy

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Thalidomide derivatives degrade BCL-2 by reprogramming the binding surface of CRBN

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PROTAC as a novel anti-cancer strategy by targeting aging-related signaling

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mRNA PROTACs: engineering PROTACs for high‐efficiency targeted protein degradation

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Design, Synthesis, and Evaluation of BCL‐2 Targeting PROTACs

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Application of proteolysis targeting chimeric (PROTAC) technology in protein regulation and drug development

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Discovery of XZ338, a highly potent BCL-XL degrader

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Discovery of PZ671, a highly potent and in vivo active CRBN-recruiting Bcl-xL degrader

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Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies

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Discovery of Dual BCL-xL/BCL-w Degraders by Exploiting the Bis(sulfonyl)benzene Ring of ABT-263 as a Linkage Vector

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Mitochondrial priming in therapy-induced senescence: implications for CAR-T/NK immunosenolytic therapy

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Mivebresib synergized with PZ703b, a novel Bcl-xl PROTAC degrader, induces apoptosis in bladder cancer cells via the mitochondrial pathway

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Computational Modeling of PROTAC Ternary Complexes and Linker Design

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A First-in-Class Dual Degrader of Bcl-2/Bcl-xL Reverses HIV Latency and Minimizes Ex Vivo Reservoirs from Patients

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The BCL-2 Family Proteins: Insights Into Their Mechanism of Action and Therapeutic Potential

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Multitargeted protein degradation: Integrating small-molecule, biomacromolecular, and nano-PROTACs for paradigm shifts in drug discovery

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Unveiling BCL-xL-specific PROTAC efficiency and dissociation pathways using native mass spectrometry

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Disrupting the MC1R/α‐MSH‐pCREB‐MITF Axis: Rhein‐based PROTAC D16 as a Potent Melanogenesis Inhibitor

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Kill Two Birds with One Stone: An Efficient and Potent AR CBS-Targeted Degrader Reverses Breast Cancer Resistance via Concurrent AR Degradation and ERα Transcriptional Suppression

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Dual-targeting Bcl-2-mediated apoptosis and synergistic pathways: Combinatorial strategies to overcome therapeutic resistance in cancer

Cheng, J., Wang, H., Zhang, Y., & Liu, G. (2026) · Biochemical Pharmacology · doi:10.1016/j.bcp.2026.117802 · Cited by 1 · see citing works

Dual FLT3/MAPK14 Proteolysis-Targeting Chimera (PROTAC) Induces Potent Acute Myeloid Leukemia Cell Death

Abdelsalam, M. A. M., Halilovic, M., Ashry, R., Nassar, H., Erdmann, F., Schmidt, M., Krämer, O. H., & Sippl, W. (2026) · Pharmaceuticals · doi:10.3390/ph19050756 · Cited by 1 · see citing works

Targeting the YY1-Bcl2-c-Myc Axis in the treatment of non-Hodgkin lymphoma

Ho, M. P., Skouradaki, E., Baritaki, S., Otumo, E., & Bonavida, B. (2025) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2025.189395 · Cited by 1 · see citing works

Discovery of Novel VEGFR-2-PROTAC Degraders Based on the Localization of Lysine Residues via Recruiting VHL for the Treatment of Gastric CancerPreprint

Wang, X. R., Wang, S., Mu, H.-X., Xu, K., Wang, X. T., Shi, J. T., Cui, Q.-H., Zhang, L. W., & Chen, S. (2022) · SSRN Electronic Journal · doi:10.2139/ssrn.4163279 · Cited by 1 · see citing works

Ginsenosides as Promising Therapeutic Agents for Glioma: Mechanisms of Action and Future Perspectives

Moftakhar, A., Najafi, S., Khoshnam, S. E., & Farzaneh, M. (2024) · Current Chemical Biology · doi:10.2174/0122127968305352240929154003

A First-in-Class Dual Degrader of Bcl-2/Bcl-xL Reverses HIV Latency and Eliminates Ex Vivo ReservoirsPreprint

Chang, L.-C., Yin, M. T., Laird, G. M., Ritter, K. D., Shah, J., & Debnath, A. K. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.10.16.618723

Synthesis and Biological Characterization of Dual-Specific Proteolysis Target Chimeras (Protacs) for the Kinases Flt3-Itd and Mapk14 with Antileukemic ActivityPreprint

Abdelsalam, M. A. M., Halilovic, M., Ashry, R., Nassar, H., Schmidt, M., Krämer, O. H., & Sippl, W. (2025) · SSRN Electronic Journal · doi:10.2139/ssrn.5336245

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

Discovery of potent indole-2-one-based BRD4 PROTACs for the treatment of acute myeloid leukemia

Wang, Z., Wang, Y., Ge, F., Zhang, J., Xiang, R., & Chen, S. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.109337

Recent advance in the targeted protein degradation technology for overcoming acute leukemia

Jin, X., Shi, Z., Liang, Z., Chen, J., Wang, C., Lou, Y., Cao, X., Zhu, L., Zhao, Y., Zhao, C., et al. (2026) · European Journal of Medicinal Chemistry Reports · doi:10.1016/j.ejmcr.2026.100331

Targeting BCL ‐ xL in Myeloid Malignancies: From Inhibitors to PROTAC

Cilloni, D., Ferrando, A., & Frassoni, F. (2026) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.71036

From Platelet Toxicity to Precision Targeting: Evolving Strategies to Overcome Thrombocytopenia in BCL‐2/BCL‐XL Inhibition

Mohiuddin, M. (2026) · Health Science Reports · doi:10.1002/hsr2.72506

BindingDB Entry 50018785: Discovery of novel VEGFR-2-PROTAC degraders based on the localization of lysine residues via recruiting VHL for the treatment of gastric cancer.

BindingDB (2024) · UC San Diego · doi:10.7270/q2tm7gcn

BindingDB Entry 50021852: Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment.

BindingDB (2025) · UC San Diego · doi:10.7270/q2v129hx

BindingDB Entry 50022871: Proline Analogues in Drug Design: Current Trends and Future Prospects.

BindingDB (2026) · UC San Diego · doi:10.7270/q2v129nq

BindingDB Entry 50021132: Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders.

BindingDB (2025) · UC San Diego · doi:10.7270/q21g0rv2

Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

Zhang, X., Thummuri, D., Liu, X., Hu, W., Zhang, P., Khan, S., Yuan, Y., Zhou, D., & Zheng, G. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112186 · Cited by 123 · see citing works

Development and crystal structures of a potent second-generation dual degrader of BCL-2 and BCL-xL

Nayak, D., Lv, D., Yuan, Y., Zhang, P., Hu, W., Nayak, A., Ruben, E. A., Lv, Z., Sung, P., Hromas, R., et al. (2024) · Nature Communications · doi:10.1038/s41467-024-46922-4 · Cited by 55 · see citing works

Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-X _L

Zhang, X., Thummuri, D., He, Y., Liu, X., Zhang, P., Zhou, D., & Zheng, G. (2019) · Chemical Communications · doi:10.1039/c9cc07217a · Cited by 86 · see citing works

Structural Insights into PROTAC-Mediated Degradation of Bcl-xL

Chung, C., Dai, H., Fernández, E., Tinworth, C. P., Churcher, I., Cryan, J., Denyer, J. C., Harling, J. D., Konopacka, A., Queisser, M. A., et al. (2020) · ACS Chemical Biology · doi:10.1021/acschembio.0c00266 · Cited by 86 · see citing works

Discovery of Dual BCL-xL/BCL-w Degraders by Exploiting the Bis(sulfonyl)benzene Ring of ABT-263 as a Linkage Vector

Poddar, S. K., Yang, Y., Pal, P., Jin, Z., Pei, J., Xiao, Y., Hu, W., Zhang, P., Adekunbi, P., Thummuri, D., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c01834 · Cited by 4 · see citing works