PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation

Sakamoto, K. M., Kim, K. B., Kumagai, A., Mercurio, F., Crews, C. M., & Deshaies, R. J. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.141230798 · Cited by 2,609

Phthalimide conjugation as a strategy for in vivo target protein degradation

Winter, G. E., Buckley, D. L., Paulk, J., Roberts, J. M., Souza, A., Dhe-Paganon, S., & Bradner, J. E. (2015) · Science · doi:10.1126/science.aab1433 · Cited by 1,760

Lymphoma incidence patterns by WHO subtype in the United States, 1992-2001

Morton, L. M., Wang, S., Devesa, S. S., Hartge, P. A., Weisenburger, D. D., & Linet, M. S. (2005) · Blood · doi:10.1182/blood-2005-06-2508 · Cited by 1,684

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

Davis, R. E., Ngo, V. N., Lenz, G., Tolar, P., Young, R. M., Romesser, P. B., Kohlhammer, H., Lamy, L., Zhao, H., Yang, Y., et al. (2010) · Nature · doi:10.1038/nature08638 · Cited by 1,651

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

Honigberg, L. A., Smith, A. M., Sirisawad, M., Verner, E., Loury, D., Chang, B., Li, S., Pan, Z., Thamm, D. H., Miller, R. A., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1004594107 · Cited by 1,561

Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

Woyach, J. A., Furman, R. R., Liu, T.-M., Ozer, H. G., Zapatka, M., Ruppert, A. S., Xue, L., Li, D. H.-H., Steggerda, S. M., Versele, M., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1400029 · Cited by 1,275

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Lu, J., Qian, Y., Altieri, M., Dong, H., Wang, J., Raina, K., Hines, J., Winkler, J. D., Crew, A. P., Coleman, K., et al. (2015) · Chemistry & Biology · doi:10.1016/j.chembiol.2015.05.009 · Cited by 1,140

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

Byrd, J. C., Harrington, B. K., O'Brien, S. M., Jones, J. A., Schuh, A., Devereux, S., Chaves, J. M., Wierda, W. G., Awan, F. T., Brown, J. R., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1509981 · Cited by 916

Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase

Pan, Z., Scheerens, H., Li, S., Schultz, B. E., Sprengeler, P. A., Burrill, L. C., Mendonca, R. V., Sweeney, M. D., Scott, K. C. K., Grothaus, P. G., et al. (2006) · ChemMedChem · doi:10.1002/cmdc.200600221 · Cited by 690

Bruton’s tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

Mohamed, A. J., Yu, L., Bäckesjö, C., Vargas, L., Faryal, R., Aints, A., Christensson, B., Berglöf, A., Vihinen, M., Nore, B. F., et al. (2009) · Immunological Reviews · doi:10.1111/j.1600-065x.2008.00741.x · Cited by 516

PROTACs: Novel approach for cancer breakdown by breaking proteins

Memon, H., & Patel, B. M. (2022) · Life Sciences · doi:10.1016/j.lfs.2022.120577 · Cited by 11

SOHO State of the Art Updates and Next Questions: Updates on BTK Inhibitors for the Treatment of Chronic Lymphocytic Leukemia

Easaw, S. M., Ezzati, S., & Coombs, C. C. (2023) · Clinical Lymphoma Myeloma & Leukemia · doi:10.1016/j.clml.2023.07.011 · Cited by 11

Proteasomal and lysosomal degradation for specific and durable suppression of immunotherapeutic targets

Wang, Y., Deng, S., & Xu, J. (2020) · Cancer Biology and Medicine · doi:10.20892/j.issn.2095-3941.2020.0066 · Cited by 10

Discovery of TQ-3959 as a Potent and Orally Bioavailable BTK PROTAC Degrader Incorporating a Novel Benzisoxazole-Based CRBN Ligand for the Treatment of B-Cell Malignancies

Ren, J., Huang, Y., Wang, J.-N., Xu, S., Wang, L., Yan, Q., Zhang, X., Wang, L., Wang, Q., Wang, X., et al. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00956 · Cited by 10

Potential application of proteolysis targeting chimera (PROTAC) modification technology in natural products for their targeted protein degradation

Gu-liang, Y., Zhong, H., Xia, X., Qi, Z., Wang, C., & Li, S. (2021) · Food Science and Human Wellness · doi:10.1016/j.fshw.2021.11.001 · Cited by 10

Exploitation of Proximity-Mediated Effects in Drug Discovery: An Update of Recent Research Highlights in Perturbing Pathogenic Proteins and Correlated Issues

Zhao, C., Wang, H., Zhan, W., Lv, X., & Ma, X. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00079 · Cited by 9

Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy

Zheng, S., Chen, R., Zhang, L., Tan, L., Li, L., Long, F., & Wang, T. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116702 · Cited by 11

Preclinical and Clinical Advances of Targeted Protein Degradation as a Novel Cancer Therapeutic Strategy: An Oncologist Perspective

Yang, X., He, Y., Kim, R. D., Fleming, J. B., & Xie, H. (2020) · Targeted Oncology · doi:10.1007/s11523-020-00782-2 · Cited by 10

Design, synthesis, and evaluation of BTK-targeting PROTACs with optimized bioavailability in vitro and in vivo

Sun, Y., Yang, Z., Zhang, Z., Li, Z., Guo, L., Pan, H., Luo, X., Liu, D. J., & Rao, Y. (2023) · RSC Medicinal Chemistry · doi:10.1039/d3md00216k · Cited by 9

Progress on Small-Molecule Proteolysis-Targeting Chimeras

Huang, W., Wang, B., Zhang, Z., Zhang, C., Zeng, S., & Shen, Z. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0161 · Cited by 10

Synthetic approaches to constructing proteolysis targeting chimeras (PROTACs)

Bakulina, O., Sapegin, A., Bunev, A. S., & Krasavin, M. (2022) · Mendeleev Communications · doi:10.1016/j.mencom.2022.07.001 · Cited by 8

Developing potent BTKC481S PROTACs for ibrutinib-resistant malignant lymphoma

Sun, Y., Luo, X., Yang, Z., Lv, W., Chen, L., Li, H., & Rao, Y. (2022) · Chinese Chemical Letters · doi:10.1016/j.cclet.2022.107924 · Cited by 8

PROTAC technology for prostate cancer treatment

Wang, Z., Zhang, D., Inuzuka, H., & Wei, W. (2025) · Acta Materia Medica · doi:10.15212/amm-2024-0075 · Cited by 9

ERα-Targeting PROTAC as a Chemical Knockdown Tool to Investigate the Estrogen Receptor Function in Rat Menopausal Arthritis

Duan, L., Xu, X. G., Xu, L., Wen, C., Ouyang, K., Li, Z., & Liang, Y. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.764154 · Cited by 8

Hydrophobic tagging-induced degradation of NAMPT in leukemia cells

Guo, M., Song, Y., Cheng, J., Dong, G., Sun, X., & Sheng, C. (2023) · Chinese Chemical Letters · doi:10.1016/j.cclet.2023.109392 · Cited by 7

Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma

Sun, Y., Liu, X., He, Q., Zhang, N., Yan, W., Lv, X., & Wang, Y. (2024) · RSC Medicinal Chemistry · doi:10.1039/d4md00252k · Cited by 7

Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer

Ying, S., Chi, H., Xiao-qiu, W., Zeng, P., Chen, J., Fu, T., Fu, W., Zhang, P., & Tan, W. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c02417 · Cited by 8

Beute für das Proteasom: Gezielter Proteinabbau aus medizinalchemischer Perspektive

Luh, L. M., Scheib, U., Juenemann, K., Wortmann, L., Brands, M., & Cromm, P. M. (2020) · Angewandte Chemie · doi:10.1002/ange.202004310 · Cited by 7

Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies

Wu, Y., Zhang, J., Zhu, X., & Zhang, Y. (2022) · Cancer Letters · doi:10.1016/j.canlet.2022.215808 · Cited by 8

Capsule-based automated synthesis for the efficient assembly of PROTAC like molecules

Bordi, S., Jiang, T., Konopka, A., Coin, G., Nichols, P. L., & Wanner, B. M. (2023) · Digital Discovery · doi:10.1039/d3dd00027c · Cited by 8

From Degraders to Molecular Glues: New Ways of Breaking Down Disease‐Associated Proteins

Nagel, Y. A., Britschgi, A., & Ricci, A. (2021) · Wiley eBooks · doi:10.1002/9783527826872.ch2 · Cited by 6

Design, synthesis, and biological evaluation of novel BTK-targeting proteolysis targeting chimeras (PROTACs) with enhanced pharmacokinetic properties

Lin, Y., Liu, J., Tian, X., Wang, J., Su, H., Xiang, J., Cao, T., Wang, Y., Xie, Q., & Yu, X. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117420 · Cited by 6

The proteolysis targeting chimera GMB-475 combined with dasatinib for the treatment of chronic myeloid leukemia with BCR::ABL1 mutants

Wu, Y., Wu, X., Wang, X., Wei, X., Tang, Y., Ouyang, X., & Gong, Y. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.931772 · Cited by 6

PROTACs: Walking through hematological malignancies

Malhab, L. J. B., AlSafar, H. S., Ibrahim, S. M., & Rahmani, M. (2023) · Frontiers in Pharmacology · doi:10.3389/fphar.2023.1086946 · Cited by 6

Targeted protein degradation in autoimmune diseases: from mechanisms to therapeutic breakthroughs

Song, Y., Zhou, B., Long, J., & Peng, Y. (2025) · Journal of Autoimmunity · doi:10.1016/j.jaut.2025.103475 · Cited by 7

Photoredox-catalyzed reaction as a powerful tool for rapid natural product Gem-dimethylation modification: discovery of potent anti-cancer agents with improved druggability

Zhang, C., Song, Y., Sun, X., Liu, Q., Li, Z., Yin, S., Xi, J., Zhai, X., & Rao, Y. (2023) · Acta Materia Medica · doi:10.15212/amm-2023-0032 · Cited by 5

Identification of a novel Azaspirooxindolinone-based PROTAC for selective BTK degradation and enhanced anticancer activity

Rampeesa, N. K., Gundla, R., Mudasani, G., Tangallapalli, S., Anugu, S. R., Gurská, S., Sanctis, J. B. D., Džubák, P., Hajdúch, M., & Das, V. (2025) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2025.108316 · Cited by 5

Synthesis and application of small molecules approved for the treatment of lymphoma

Guo, Y., Zhang, J., Sun, J., Nie, P., & Gao, H. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115835 · Cited by 5

Resistance Mechanism for Zanubrutinib in Marginal Zone Lymphoma

Sharp, J., Shana’ah, A. Y., Voorhees, T. J., Bond, D. A., Sawalha, Y., Sigmund, A. M., Hanel, W. G., Sehgal, L., Alinari, L., Baiocchi, R. A., et al. (2025) · Journal of the National Comprehensive Cancer Network · doi:10.6004/jnccn.2025.7045 · Cited by 4

Design, synthesis and biological evaluation of MNK-PROTACs

Sun, X., Wu, Q., Bu, H., Pei, Y., Guan, D., Guo, S., Zhou, J., & Zhang, H. (2024) · Molecular Diversity · doi:10.1007/s11030-023-10776-7 · Cited by 4

Advantages and Disadvantages of PROTACs

Pujari, R., Bhatt, S., Soni, U., Sharma, S., & Patil, S. (2024) · Springer eBooks · doi:10.1007/978-981-97-5077-1_4 · Cited by 4

Recent Advances in the Development of RET Inhibitors

Lu, P., Qin, H., Ye, J., Chen, P., Li, J., Ren, J., Wang, Y., & Zhang, Y. (2023) · Letters in Drug Design & Discovery · doi:10.2174/1570180820666230306113551 · Cited by 4

Discovery of novel PROTACs based on multi-targeted angiogenesis inhibitors

Si, R., Hai, P., Zheng, Y., Liu, N., Wang, J., Zhang, Q., Li, Y., Pan, X., & Zhang, J. (2023) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2023.129275 · Cited by 4

Significance of Selective Protein Degradation in the Development of Novel Targeted Drugs and Its Implications in Cancer Therapy

Yang, J., Wang, Q.-L., Feng, G., & Zeng, M. (2020) · Advanced Therapeutics · doi:10.1002/adtp.201900210 · Cited by 4

Computational Modeling of PROTAC Ternary Complexes and Linker Design

Miller, S. A., Andrianov, G. V., Mischley, V., Wharton, K. A., Chen, J. J., & Karanicolas, J. (2022) · Wiley eBooks · doi:10.1002/9783527836208.ch5 · Cited by 4

Bruton Tyrosine Kinase Degraders in B-Cell Malignancies

Huynh, T., Rodrı́guez, S., & Danilov, A. V. (2024) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-23-0520 · Cited by 4

Preclinical Studies of PROTACs in Hematological Malignancies

Fuchs, O., & Bokorová, R. (2021) · Cardiovascular & Haematological Disorders - Drug Targets · doi:10.2174/1871529x21666210308111546 · Cited by 3

Predicting PROTAC-targeted Degradation and Designing Androgen Receptor Degraders with AiPROTACPreprint

Zhang, L., Sun, R., Li, X., Ren, C., Long, Y., Tan, W., Wang, X., Zou, K., Yang, X., Wu, M., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.02.26.640266 · Cited by 5

Design and evaluation of selective BET PROTACs with potent antitumor efficacy and safety against acute myeloid leukemia

Wei, Q., Zhang, J., Chen, J., Cai, X., 周金培, Wang, B., Zhang, H., & Cao, P. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.118667 · Cited by 2

Discovery of a Potent NAMPT-Targeting PROTAC for the Suppression of Triple-Negative Breast Cancer via Macrophage Reprogramming

Song, Y., Yang, C., Li, Q., Huang, S., Chen, S., Xia, Z., Yao, X., Sheng, C., & Dong, G. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00454 · Cited by 2

Targeted protein degradation: bridging chemical biology and clinical translation

Zhang, Y., Fu, J.-W., Liu, Y., Wu, R. Y., Liang, Y., Zhang, W., Yuan, T., Zhu, H., He, Q.-J., & Yang, B. (2026) · Acta Pharmacologica Sinica · doi:10.1038/s41401-026-01861-2 · Cited by 2

C-MET tyrosine kinase receptor: mechanisms, clinical applications and future perspectives in cancer therapy

Zhu, C., Li, Y., Xu, H., Sun, L., Wei, Y., 马承娴, Chen, Q., & He, X. (2026) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-026-02682-9 · Cited by 4

Combating relapsed and refractory Mantle cell lymphoma with novel therapeutic armamentarium: Recent advances and clinical prospects

Raghani, N. R., Shah, D. D., Shah, T. S., Chorawala, M. R., & Patel, R. B. (2023) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2023.104085 · Cited by 3

Screening and Characterization of Allosteric Small Molecules Targeting Bruton’s Tyrosine Kinase

Kueffer, L. E., Lin, D. Y.-W., Amatya, N., Serrenho, J., Joseph, R. E., Courtney, A. H., & Andreotti, A. H. (2023) · Biochemistry · doi:10.1021/acs.biochem.3c00362 · Cited by 3

4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry

Chen, X., Huang, Y., Xu, W., Cai, Y., & Yang, Y. (2022) · RSC Medicinal Chemistry · doi:10.1039/d2md00139j · Cited by 2

Targeted Protein Degradation by Proteolysis Targeting Chimeras

Du, W. (2022) · Wiley eBooks · doi:10.1002/9781119627784.ch11 · Cited by 2

Three targets in 1 shot against ibrutinib resistance

Chiron, D. (2019) · Blood · doi:10.1182/blood-2018-12-892760 · Cited by 1

Enzyme‐Activated Orthogonal Proteolysis Chimeras for Tumor Microenvironment‐Responsive Immunomodulation

Sun, C., Liu, S., Lau, J. W., Yang, H., Chen, Y., & Xing, B. (2025) · Angewandte Chemie · doi:10.1002/ange.202423057 · Cited by 1

From C481 Resistance Evasion to Platelet Preservation: Rilzabrutinib Redefines ITP Targeted Therapy

Liu, L., Xiao, Y., Jia, Y., Shao, Z., Shi, J., & Cui, C. (2025) · Drug Design Development and Therapy · doi:10.2147/dddt.s543620 · Cited by 1

Bifunctional proximity-inducing strategies for targeted and programmable post-translational modifications

Tanga, S., Das, P., Samoi, T. B., Hota, A., Karmakar, A., & Maji, B. (2026) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2026.115874 · Cited by 1

Synthesis of RARα–PROTAC and its delivery via Polygonatum sibiricum exosome-like nanoparticles for the treatment of colorectal cancer

Zhu, G., Zhao, Y., Chen, M., Lu, S., Xu, L., Chen, G., Zeng, L., & Chen, J. (2026) · Materials Today Bio · doi:10.1016/j.mtbio.2026.103651 · Cited by 1

Using Informatics Tools to Identify Opportunities for Precision Medicine in Diffuse Large B-cell Lymphoma

Patel, S. P., Harkins, R. A., Lee, M. J., Flowers, C. R., & Koff, J. L. (2019) · Clinical Lymphoma Myeloma & Leukemia · doi:10.1016/j.clml.2019.12.003 · Cited by 1

Targeted Protein Degradation Chemical Probes

Galdeano, C., & Barril, X. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160745-00150 · Cited by 1

[Advances in clinical research on novel BTK inhibitors for the treatment of chronic lymphocytic leukemia].

Qiu, T., Miao, Y., & Li, J. Y. (2023) · PubMed Central · doi:10.3760/cma.j.issn.0253-2727.2023.11.015 · Cited by 1

Racial and Ethnic Characteristics and Outcomes of Patients Diagnosed with CLL/SLL in the USA

Bruno, D. S., Khanal, M., Li, X. I., Escalón, M. P., Winfree, K. B., & Hess, L. M. (2024) · Acta Haematologica · doi:10.1159/000538836 · Cited by 1

Proteolysis-targeting chimeras (PROTACs) as novel biotechnology for cancer therapy

Fuchs, O. (2022) · Elsevier eBooks · doi:10.1016/b978-0-323-90042-3.15001-7 · Cited by 1

Targeted KRAS G12V degradation elicits efficient and durable lung adenocarcinoma regression in vivoPreprint

Martín, A. J. M., García-Pérez, I. M., José, S. S., Rojo, P., Riego‐Mejías, C., Teodósio, C., Barbosa, B. M. G., Sánchez, C., Folch-I-Casanovas, I., Caballol, A. O., et al. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.12.13.627539 · Cited by 1

Defeating kinases that promote tumorigenesis through non-catalytic functions with PROTACs - PIM kinase as an example

Torres‐Ayuso, P., & Brognard, J. (2025) · Expert Opinion on Therapeutic Targets · doi:10.1080/14728222.2025.2500418 · Cited by 1

PROTAC Targeting BTK for the Treatment of Ibrutinib-resistant B-cell Malignancies

Sun, Y., & Rao, Y. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160691-00147

Progress in the Research of Kinases PROTAC

陈, 泉. (2022) · Hans Journal of Medicinal Chemistry · doi:10.12677/hjmce.2022.101002

Proteolysis-targeting Chimeras Technology for Selective Protein Degradation

Xia, Y. (2021) · Cancer Cell Research · doi:10.54762/ccr2021.795-806

Multi‐Specific Binding Strategy

Zhou, Y., Xu, S., Ding, D., Tang, K., Liu, X., Kim, M., & Zhan, P. (2024) · Wiley eBooks · doi:10.1002/9781394182862.ch11

Development of visible-light photocaged molecular glues (vc-MGs) for B-cell malignancies therapy with improved safety and pharmacokinetic profiles in vivo

Yan, W., Zhang, N., Liu, X., He, Q., Lv, X., Sun, J., Zhuang, L., Zou, Y., Liang, Y., Liang, Y., et al. (2025) · Chinese Chemical Letters · doi:10.1016/j.cclet.2025.112064

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

Additional file 1 of Degradation of neurodegenerative disease-associated TDP-43 aggregates and oligomers via a proteolysis-targeting chimera

Tseng, Y.-L., Lu, P.-C., Lee, C.-C., He, R.-Y., Huang, Y.-A., Tseng, Y.-C., Cheng, T.-J. R., Huang, J. J.-T., & Fang, J.-M. (2024) · Figshare · doi:10.6084/m9.figshare.26584962

Applications of Precise Chemistry in Drug Discovery★

Liu, R., Zuo, Y., Zhang, Y., & Zhang, J. (2025) · Chinese Journal of Organic Chemistry · doi:10.6023/cjoc20205031

MDM2 Amplification Enables Selective PROTAC Targeting of Tumor Cells

Fatima, Z., Chen, L., Yin, M., Cui, Y., Cai, J., & Chen, J. (2026) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-25-0990

PROTAC-Mediated Ternary Complex Stability with Ricin Toxin A: A Computational Perspective

Botelho, F. D., Islam, S. T., LaPlante, S. R., & França, T. C. C. (2026) · ACS Omega · doi:10.1021/acsomega.5c10223

PROTAC-mediated regulation of programmed cell death: From molecular mechanisms to therapeutic breakthroughs

Huang, H., Deng, A., Pan, F., Lu, Y., Chen, L., Cao, J., Tang, Q., Liu, Y., Wu, Y., Du, J., et al. (2026) · The Innovation · doi:10.1016/j.xinn.2026.101359

Etude du rôle du récepteur aux hydrocarbures aromatiques au niveau de la physiologie cutanée

Coatmeur, R. (2022) · theses.fr (ABES) · doi:10.70675/b9195e66z1ff5z48f7z84e5z392c50dd13ec

Design and synthesis of trisubstituted 1,2,4-triazoles : structural exploration in the inhibition of GSK-3β for the treatment of Alzheimer’s disease

Pereira, T. M. (2024) · theses.fr (ABES) · doi:10.70675/f501300bz5a57z477eza236z79f3a6d2a052

New Generations of Antibodies and Scaffold Proteins as a Way to Create Highly Selective Conjugates for Oncology

Shulcheva, I. V., & Ulitin, A. B. (2026) · Biomedical Chemistry Research and Methods · doi:10.18097/bmcrm00305

Kinase degrader: a new era of drug development

Zhang, C., & Rao, Y. (2026) · Elsevier eBooks · doi:10.1016/b978-0-443-43974-2.00004-5

PROTACs: Next-generation cancer therapeutics revolutionizing targeted treatment strategies

Sireen, U., Thota, S., Amreen, N., Kumaraswamy, D., Katherashala, S., & Sriram, S. (2026) · In Silico Research in Biomedicine · doi:10.1016/j.insi.2026.100386

Research progress of proteolysis-targeting chimeras in viral hepatitis drug discovery

Hao, X., Wang, Y., Huang, G., Lin, C., Zhao, P., Zhi, W., Li, X., Qi, P., & Liu, P. (2026) · Frontiers in Chemistry · doi:10.3389/fchem.2026.1810498

Hunting gremlins: GREM1 as a new therapeutic target for multiple diseases including glaucoma

Siderovski, D. P., Myneni, N., Botross, M., Patel, P. D., & Clark, A. F. (2026) · Pharmacological Reviews · doi:10.1016/j.pharmr.2026.100152

Regulation of different kinases for Alzheimer's disease therapy: progresses and perspectives

Han, M., Liao, Q., He, S., Guo, L., Lu, Z., Wang, X., Sun, W., Duan, Y. B., Lyu, W., & Li, Q. (2026) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2026.110300

Targeted protein degradation technologies for modulating cell-cell communication

Lu, Y., & Wang, M. (2026) · Scientia Sinica Chimica · doi:10.1360/ssc-2026-0145

Development of chimeric molecules from isoindolinone derivatives

Григорьева, Т. А., Sokolova, A. N., Nechepurenko, D. A., Romanova, A. A., & Tribulovich, V. G. (2026) · Russian Chemical Bulletin · doi:10.1007/s11172-026-5012-4

Beyond the ATP-binding pocket: emerging strategies in kinase targeting from allosteric inhibition to targeted protein degradation

Zhou, M., Li, L., Tang, X., Zhao, Y., & Zhang, W. (2026) · Future Medicinal Chemistry · doi:10.1080/17568919.2026.2718758

Proteolysis Targeting Chimera (PROTAC) Linkerology Enhances the CDK-Degradation Selectivity Profile of a Multi-CDK Inhibitor: Discovery of Potent, Anti-Leukemic CDK9 Degraders

Chan, A. M., Eberly, C. L., Goodis, C. C., Nordquist, E. B., Weldemariam, M. M., Carter‐Cooper, B., Pogash, S., Lapidus, R. S., Kane, M. A., MacKerell, A. D., et al. (2026) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.6c00232

Targeted degradation of protein in hematologic malignancies: mechanisms, therapeutic strategies, and clinical prospects

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Emerging drug profile: bexobrutideg

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Rational design and synthesis of a novel cereblon ligand class enabling selective molecular glue and potent PROTAC

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BindingDB Entry 50014952: Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs.

BindingDB (2023) · UC San Diego · doi:10.7270/q2bp06p2

BindingDB Entry 50022808: Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy.

BindingDB (2026) · UC San Diego · doi:10.7270/q2bc44cm

BindingDB Entry 50012690: Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.

BindingDB (2022) · UC San Diego · doi:10.7270/q2g73jdh

BindingDB Entry 50010738: Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein.

BindingDB (2021) · UC San Diego · doi:10.7270/q2nz8c6f

BindingDB Entry 50011293: Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.

BindingDB (2022) · UC San Diego · doi:10.7270/q2gm8bxf

BindingDB Entry 50016776: Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma.

BindingDB (2023) · UC San Diego · doi:10.7270/q2s186hb

BindingDB Entry 50016318: Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.

BindingDB (2023) · UC San Diego · doi:10.7270/q2fx7fhq

BindingDB Entry 50018749: PROTAC: A promising technology for cancer treatment.

BindingDB (2024) · UC San Diego · doi:10.7270/q2q244hq

BindingDB Entry 50018664: Progress in the development of small molecular inhibitors of the Bruton's tyrosine kinase (BTK) as a promising cancer therapy.

BindingDB (2024) · UC San Diego · doi:10.7270/q2v410fz

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

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

BindingDB Entry 50010796: Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer.

BindingDB (2021) · UC San Diego · doi:10.7270/q2rn3cfh

BindingDB Entry 50018682: 4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.

BindingDB (2024) · UC San Diego · doi:10.7270/q25b06rz

BindingDB Entry 50019487: The current strategies of optimization of oseltamivir against mutant neuraminidases of influenza A：A review.

BindingDB (2024) · UC San Diego · doi:10.7270/q24m98xw

BindingDB Entry 50022437: Synthesis and application of small molecules approved for the treatment of lymphoma.

BindingDB (2025) · UC San Diego · doi:10.7270/q25q51tg

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PROTAC Targeting BTK for the Treatment of Ibrutinib-resistant B-cell Malignancies

Sun, Y., & Rao, Y. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160691-00147

Bruton's tyrosine kinase inhibitors in B‐cell non‐Hodgkin's lymphomas

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