Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: A novel approach to activate Nrf2 function

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p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming

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Discovery of direct inhibitors of Keap1–Nrf2 protein–protein interaction as potential therapeutic and preventive agents

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Discovery of Potent Keap1–Nrf2 Protein–Protein Interaction Inhibitor Based on Molecular Binding Determinants Analysis

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Discovery of a small-molecule inhibitor and cellular probe of Keap1–Nrf2 protein–protein interaction

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Keap Calm, and Carry on Covalently

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Nrf2 and Cardiovascular Defense

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The Keap1/Nrf2 pathway in health and disease: from the bench to the clinic

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Rapid Identification of Keap1–Nrf2 Small-Molecule Inhibitors through Structure-Based Virtual Screening and Hit-Based Substructure Search

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Peptide inhibitors of the Keap1–Nrf2 protein–protein interaction

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Druggability Assessment of Protein–Protein Interfaces

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Polar Recognition Group Study of Keap1-Nrf2 Protein–Protein Interaction Inhibitors

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Design, Synthesis, and Initial Evaluation of Affinity-Based Small-Molecule Probes for Fluorescent Visualization and Specific Detection of Keap1

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Nrf2 and Oxidative Stress: A General Overview of Mechanisms and Implications in Human Disease

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Nrf2/Keap1/ARE signaling: Towards specific regulation

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Interfering peptides targeting protein–protein interactions: the next generation of drugs?

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Anti-Viral Potential and Modulation of Nrf2 by Curcumin: Pharmacological Implications

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Theoretical Study of the Antioxidant Activity of Quercetin Oxidation Products

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Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors

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Discovery of a head-to-tail cyclic peptide as the Keap1-Nrf2 protein-protein interaction inhibitor with high cell potency

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Targeting the NRF2 pathway for disease modification in neurodegenerative diseases: mechanisms and therapeutic implications

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Direct inhibition of Keap1-Nrf2 Protein-Protein interaction as a potential therapeutic strategy for Alzheimer's disease

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Leonurine ameliorates D-galactose-induced aging in mice through activation of the Nrf2 signalling pathway

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Identification of a novel small-molecule Keap1–Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy

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A potent phosphodiester Keap1-Nrf2 protein-protein interaction inhibitor as the efficient treatment of Alzheimer's disease

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Emerging Screening Approaches in the Development of Nrf2–Keap1 Protein–Protein Interaction Inhibitors

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Nrf2, the Major Regulator of the Cellular Oxidative Stress Response, is Partially Disordered

Karunatilleke, N. C., Fast, C. S., Ngo, V., Brickenden, A. M., Duennwald, M. L., Konermann, L., & Choy, W. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22147434 · Cited by 52 · see citing works

Design, Synthesis, and Structure–Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein–Protein Interaction Inhibitors

Zhou, H.-S., Hu, L.-B., Zhang, H., Shan, W.-X., Wang, Y., Li, X., Liu, T., Zhao, J., You, Q., & Jiang, Z. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01116 · Cited by 49 · see citing works

A bioactive ligand-conjugated iridium(III) metal-based complex as a Keap1–Nrf2 protein-protein interaction inhibitor against acetaminophen-induced acute liver injury

Li, G., Liu, H., Feng, R., Kang, T., Wang, W., Ko, C.-N., Wong, C., Ye, M., Ma, D., Wan, J., et al. (2021) · Redox Biology · doi:10.1016/j.redox.2021.102129 · Cited by 44 · see citing works

Recapitulating the Binding Affinity of Nrf2 for KEAP1 in a Cyclic Heptapeptide, Guided by NMR, X-ray Crystallography, and Machine Learning

Ortet, P. C., Muellers, S. N., Viarengo‐Baker, L. A., Streu, K., Szymczyna, B. R., Beeler, A. B., Allen, K. N., & Whitty, A. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.0c09799 · Cited by 45 · see citing works

Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy

Ayoup, M. S., Abu-Serie, M. M., Abdel‐Hamid, H., & Teleb, M. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113475 · Cited by 43 · see citing works

Understanding the Emerging Link Between Circadian Rhythm, Nrf2 Pathway, and Breast Cancer to Overcome Drug Resistance

Bevinakoppamath, S., Ramachandra, S. C., Yadav, A. K., Basavaraj, V., Vishwanath, P., & Prashant, A. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.719631 · Cited by 42 · see citing works

Cyclovirobuxine D protects against diabetic cardiomyopathy by activating Nrf2-mediated antioxidant responses

Jiang, Z., Fu, L., Xu, Y., Hu, X., Yang, H., Zhang, Y., Luo, H., Gan, S., Tao, L., Liang, G., et al. (2020) · Scientific Reports · doi:10.1038/s41598-020-63498-3 · Cited by 42 · see citing works

Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1–Nrf2) Protein–Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity

Lu, M., Zhang, X., Wu, F., Tan, S.-J., Zhao, J., You, Q., & Jiang, Z. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00818 · Cited by 41 · see citing works

A hydrogen peroxide responsive prodrug of Keap1-Nrf2 inhibitor for improving oral absorption and selective activation in inflammatory conditions

Lu, M., Zhang, X., Zhao, J., You, Q., & Jiang, Z. (2020) · Redox Biology · doi:10.1016/j.redox.2020.101565 · Cited by 41 · see citing works

Role of NRF2 in Pathogenesis of Alzheimer’s Disease

Chu, C., Uruno, A., Katsuoka, F., & Yamamoto, M. (2024) · Antioxidants · doi:10.3390/antiox13121529 · Cited by 43 · see citing works

Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors

Wang, Y., Ma, H., Huang, J., Yao, Z., Yu, J., Zhang, W., Zhang, L., Wang, Z., & Zhuang, C. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.113030 · Cited by 38 · see citing works

Crystallography-Guided Optimizations of the Keap1–Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides

Liu, G., Hou, R., Xu, L., Zhang, X., Yan, J., Xing, C., Xu, K., & Zhuang, C. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00170 · Cited by 37 · see citing works

Natural Product-Inspired Targeted Protein Degraders: Advances and Perspectives

Li, J., Cai, Z., Li, X., & Zhuang, C. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01223 · Cited by 37 · see citing works

Fragment-growing guided design of Keap1-Nrf2 protein-protein interaction inhibitors for targeting myocarditis

Meng, N., Tang, H., Zhang, H., Jiang, C., Su, L., Min, X., Zhang, W., Zhang, H., Miao, Z., Zhang, W., et al. (2018) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2018.02.010 · Cited by 36 · see citing works

Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury

Zhang, L., Xu, L., Chen, H., Zhang, W., Xing, C., Qu, Z., Yu, J., & Zhuang, C. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113599 · Cited by 35 · see citing works

Novel diterpenoid-type activators of the Keap1/Nrf2/ARE signaling pathway and their regulation of redox homeostasis

Li, A., Shen, T., Wang, T. Z., Zhou, M., Wang, B., Song, J., Zhang, P.-L., Wang, X., Ren, D., Lou, H., et al. (2019) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2019.06.001 · Cited by 32 · see citing works

NRF2-mediated regulation of lipid pathways in viral infection

Muzammil, K., Ghnim, Z. S., Gataa, I. S., Al-Hussainy, A. F., Soud, N. A., Adil, M., Shallan, M. A., & Yasamineh, S. (2024) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2024.101279 · Cited by 29 · see citing works

Corylin from Psoralea fructus ( Psoralea corylifolia L.) protects against UV ‐induced skin aging by activating Nrf2 defense mechanisms

Li, N., Liu, T., Zhu, S., Yang, Y. A., Wang, Z., Zhao, Z., Liu, T., Wang, X., Qin, W., Yan, Y., et al. (2022) · Phytotherapy Research · doi:10.1002/ptr.7501 · Cited by 28 · see citing works

Medicinal Chemistry Insights into the Development of Small-Molecule Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1–Nrf2) Protein–Protein Interaction Inhibitors

Zhao, Z., Dong, R., You, Q., & Jiang, Z. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00712 · Cited by 28 · see citing works

Structure-activity relationships of 1,4-bis(arylsulfonamido)-benzene or naphthalene-N,N′-diacetic acids with varying C2-substituents as inhibitors of Keap1-Nrf2 protein-protein interaction

Lee, S., Abed, D. A., Nguyen, M.-U., Verzi, M. P., & Hu, L. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114380 · Cited by 27 · see citing works

Modulation of NRF2/KEAP1-Mediated Oxidative Stress for Cancer Treatment by Natural Products Using Pharmacophore-Based Screening, Molecular Docking, and Molecular Dynamics Studies

Alzain, A. A., Mukhtar, R. M., Abdelmoniem, N., Shoaib, T. H., Osman, W., Alsulaimany, M., Aljohani, A. K. B., Almadani, S. A., Alsaadi, B., Althubyani, M. M., et al. (2023) · Molecules · doi:10.3390/molecules28166003 · Cited by 27 · see citing works

A cell-active cyclic peptide targeting the Nrf2/Keap1 protein–protein interaction

Iegre, J., Krajčovičová, S., Gunnarsson, A., Wissler, L., Käck, H., Łuchniak, A., Tångefjord, S., Narjes, F., & Spring, D. R. (2023) · Chemical Science · doi:10.1039/d3sc04083f · Cited by 26 · see citing works

NRF2 in dermo‐cosmetic: From scientific knowledge to skin care products

Frantz, M., Rozot, R., & Marrot, L. (2022) · BioFactors · doi:10.1002/biof.1907 · Cited by 26 · see citing works

Computational investigation of quinazoline derivatives as Keap1 inhibitors for Alzheimer's disease

Gote, S. A., Thapa, S., Dubey, S., Nargund, S. L., & Biradar, M. S. (2023) · Informatics in Medicine Unlocked · doi:10.1016/j.imu.2023.101334 · Cited by 22 · see citing works

Gamma-oryzanol alleviates osteoarthritis development by targeting Keap1–Nrf2 binding to interfere with chondrocyte ferroptosis

Dai, Z.-H., Zhou, C.-C., Yu, C., Qian, C., Jin, S., Du, S.-Q., Lv, Y.-Y., Jin, C., Zheng, G., & Zhan, Y. (2024) · International Immunopharmacology · doi:10.1016/j.intimp.2023.111469 · Cited by 16 · see citing works

Terpenoids from stigma maydis (Zea mays L.) alleviate hydrogen peroxide-induced SH-SY5Y cell injury by activating Nrf2

Song, X., Guo, R., Qi, X., Feng-ying, H., Lin, B., Huang, X., Yao, G., & Song, S. (2020) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2020.104131 · Cited by 16 · see citing works

Nrf2 signaling activation by a small molecule activator compound 16 inhibits hydrogen peroxide-induced oxidative injury and death in osteoblasts

Zhao, J., Tang, P., Zhou, Z., Xu, G., Li, Q., Li, K.-R., & Zheng, Y. (2022) · Cell Death Discovery · doi:10.1038/s41420-022-01146-7 · Cited by 15 · see citing works

Medicinal Chemistry Strategies for the Development of Inhibitors Disrupting β-Catenin’s Interactions with Its Nuclear Partners

Zhang, H., Liu, C., Zhu, D., Zhang, Q., & Li, J. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01016 · Cited by 15 · see citing works

Discovery of a coumarin derivative as Nrf2 activator mitigating oxidative stress and fibrosis in mesangial cells under high glucose

Yao, H., Zhang, N., Zhang, W., Li, J., Hua, H., & Li, Y. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127490 · Cited by 14 · see citing works

High Throughput Screening in Drug Discovery: Problems and Solutions

Hushpulian, D. M., Gaisina, I. N., Nikulin, S. V., Chubar, T. A., Сергеевич, С. С., Gazaryan, I. G., & Tishkov, V. I. (2024) · Moscow University Chemistry Bulletin · doi:10.3103/s0027131424700081 · Cited by 14 · see citing works

Neuroprotective effect of a Keap1-Nrf2 Protein-Protein Inter-action inhibitor on cerebral Ischemia/Reperfusion injury

Qi, Z., Tong, Y., Luo, H., Chen, M., Zhou, N., & Chen, L. (2023) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2023.106350 · Cited by 13 · see citing works

Molecular basis of the interactions between the disordered Neh4 and Neh5 domains of Nrf2 and CBP /p300 in oxidative stress response

Karunatilleke, N. C., Brickenden, A. M., & Choy, W. (2024) · Protein Science · doi:10.1002/pro.5137 · Cited by 13 · see citing works

Novel Hydrogen Sulfide Hybrid Derivatives of Keap1-Nrf2 Protein–Protein Interaction Inhibitor Alleviate Inflammation and Oxidative Stress in Acute Experimental Colitis

Zhang, X., Cui, K., Wang, X., Tong, Y., Liu, C., Zhu, Y., You, Q., Jiang, Z., & Guo, X. (2023) · Antioxidants · doi:10.3390/antiox12051062 · Cited by 13 · see citing works

Navigating the complexities of neuronal signaling and targets in neurological disorders: From pathology to therapeutics

Choudhary, D., Khan, M. I., Khan, Z., Mehan, S., Gupta, G. D., Narula, A. S., & Samant, R. (2025) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2025.177417 · Cited by 13 · see citing works

Development of an enzyme-linked immunosorbent assay for Keap1-Nrf2 interaction inhibitors identification

Wang, Y., Xiao, C., Lin, H., Hu, J., Ip, T.-M., & Wan, D. C. (2020) · Redox Biology · doi:10.1016/j.redox.2020.101573 · Cited by 12 · see citing works

Design of anti-depressant phosphodiester amino acidic Keap1-Nrf2 protein-protein interaction inhibitors

Sun, Y., Wang, J., Ding, W., Qin, Q., Wang, R., Yu, R., Yan, J., Hou, R., Liu, G., Cai, X., et al. (2025) · Redox Biology · doi:10.1016/j.redox.2025.103620 · Cited by 11 · see citing works

Discovery of polypodiside as a Keap1-dependent Nrf2 activator attenuating oxidative stress and accumulation of extracellular matrix in glomerular mesangial cells under high glucose

Yao, H., Zhang, N., Zhang, W., Li, J., Hua, H., & Li, Y. (2020) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2020.115833 · Cited by 10 · see citing works

Discovery of β-amino acid substituted naphthalene sulfonamide derivatives as potent Kelch-like ECH-associated protein 1−nuclear factor erythroid 2-related factor 2 (Keap1−Nrf2) protein−protein interaction inhibitors for ulcerative colitis management

Zhao, Z., Lu, H., Wang, J., Wu, T., Xu, S., Ge, Y., You, Q., Jiang, Z., & Lu, M. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117384 · Cited by 8 · see citing works

Melatonin Alleviates MBP-Induced Oxidative Stress and Apoptosis in TM3 Cells via the SIRT1/PGC-1α Signaling Pathway

Liu, J., Guan, Q., Li, S., Qi, Q., & Pan, X. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26125910 · Cited by 8 · see citing works

Flavonoids from Polygonum hydropiper L. regulate PCV2-induced oxidative stress of RAW264.7 cells via Pi3k/AKT and Nrf2/HO-1 signaling pathways

Chen, Q., Wang, Q., Zhao, Y., Xie, X., Feng, H., Wei, Y., Yu, M., Pan, X., & Hu, T. (2025) · Scientific Reports · doi:10.1038/s41598-025-14362-9 · Cited by 8 · see citing works

CB5712809, a novel Keap1 inhibitor upregulates SQSTM1/p62 mediated Nrf2 activation to induce cell death in colon cancer cells

Dera, A. A., & Fayi, M. S. A. (2025) · Discover Oncology · doi:10.1007/s12672-025-02787-7 · Cited by 7 · see citing works

Tipping the balance: NRF2’s dual role in ferroptotic fate

de Souza, I., Teixeira, A. B. D. S., dos Santos, A. F., Angeli, J. P. F., & Rocha, C. R. R. (2026) · Oncogenesis · doi:10.1038/s41389-026-00630-4 · Cited by 7 · see citing works

A Multifunctional (-)-Meptazinol-Serotonin Hybrid Ameliorates Oxidative Stress-Associated Apoptotic Neuronal Death and Memory Deficits via Activating the Nrf2/Antioxidant Enzyme Pathway

Zhao, F., Zhao, L., Zhou, Y., Tan, X., Yang, Y., Ni, W., Zheng, W., Chen, H., Qiu, Y. L., & Li, J. (2023) · Oxidative Medicine and Cellular Longevity · doi:10.1155/2023/6935947 · Cited by 7 · see citing works

Comparative Molecular Profiling and Bioactivity Analysis of Algerian Propolis: Antioxidant, Antibacterial Activities, and In Silico NRF2-KEAP1 Pathway Modulation

Reguig, A., Messaï, A., Bedaida, I. K., Pinto, D. C. G. A., Bensouıcı, C., Ouamane, A. T., Silva, A. M. S., & Roy, J. (2025) · Current Issues in Molecular Biology · doi:10.3390/cimb47090761 · Cited by 5 · see citing works

Eucalyptol potentiates antianginal effect while blunts tachycardia of nifedipine in rats via nitric oxide, antioxidant, and anti-inflammatory pathways: In vivo and in vitro study

Murad, H. A. S., & Alqurashi, T. M. A. (2024) · Journal of Functional Foods · doi:10.1016/j.jff.2024.106019 · Cited by 5 · see citing works

Neuroprotective Effects of a 3-Amino Quinazoline Derivative via Keap1–Nrf2 Pathway Activation in an ICV-STZ-Induced Rat Model of Sporadic Alzheimer’s Disease

Maheta, P., Patel, C. A., Parmar, D., Beladiya, J., Patel, S. K., Sheth, D. B., & Dholakia, S. P. (2025) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.5c00540 · Cited by 4 · see citing works

Licochalcone E inhibits trxR1 expression, alters Nrf2/ STAT6 signal, and induces antitumor effects in vitro against human SH‐SY5Y and SK‐N‐BE (2) neuroblastoma cells

Zhang, Q., Zhang, J., Liu, B., & Wei, J. (2022) · Environmental Toxicology · doi:10.1002/tox.23474 · Cited by 4 · see citing works

Lupeol Attenuates Oxysterol-Induced Dendritic Cell Activation Through NRF2-Mediated Antioxidant and Anti-Inflammatory Effects

Saha, S., Capozzi, A., Profumo, E., Alessandri, C., Sorice, M., Saso, L., & Buttari, B. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26157179 · Cited by 3 · see citing works

Identification and Characterization of ERK2 Dimerization Inhibitors by Integrated In Silico and In Vitro Screening

Ortiz-González, C., Casar, B., Gozalbes, R., Serrano‐Candelas, E., Crespo, P., & Carpio, L. E. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms262311481 · Cited by 3 · see citing works

Small Molecule Inhibitors Targeting New Targets of Protein-Protein Interactions

Yue, L., Wan, W., Xu, P., Li, L., Wang, C., Zhang, Y., Xu, H., Zhang, R., Hu, J., Lu, W., et al. (2018) · Springer eBooks · doi:10.1007/978-981-13-0773-7_7 · Cited by 2 · see citing works

Development of Novel Nrf2/ARE Inducers Bearing Pyrazino[2,1-a]isoquinolin Scaffold with Potent In Vitro Efficacy and Enhanced Physicochemical Properties

Dai, H., Jiao, Q., Liu, T., You, Q., & Jiang, Z. (2017) · Molecules · doi:10.3390/molecules22091541 · Cited by 2 · see citing works

Virtual Prediction of The Effect Phenolic And Glucosinolate Compounds In Broccoli (Brassica Oleracea) On Anti-aging As Stimulant Nrf-2

Hikmawati, V. F., Alam, F. M., Ainnayah, J. S., & Fatchiyah, F. (2021) · The Journal of Experimental Life Sciences · doi:10.21776/ub.jels.2020.010.02.05 · Cited by 2 · see citing works

HIGH THROUGHPUT SCREENING IN DRUG DISCOVERY: PROBLEMS AND SOLUTIONS

Hushpulian, D. M., Gaisina, I. N., Nikulin, S. V., Chubar, T. A., Сергеевич, С. С., Gazaryan, I. G., & Tishkov, V. I. (2024) · Lomonosov chemistry journal · doi:10.55959/su0579-9384-2-2024-65-2-96-112 · Cited by 1 · see citing works

Design of spiro-heterocyclic substituted diaminonaphthalene Keap1-Nrf2 protein-protein interaction inhibitors as novel anti-depressant agents

Chen, Y., Qin, Q., Ding, W., Yu, R., Wang, R., Ji, H., Yan, J., Ma, H., Jiang, C., Sun, Y., et al. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117848 · Cited by 2 · see citing works

Antioxidant Properties of Novel Lipophilic Fluoroquinolone Compounds Against Oxidative Stress Induced by Acetaminophen and Carbon Tetrachloride in Male Wistar Rats

Alwahsh, M., Shawaqfeh, B., Alejel, R., Hasan, A., Yousef, D., Saqallah, F. G., Al-Kouz, S., Alassi, A., Swaiss, Y., Al-Hiari, Y. M., et al. (2026) · Biomolecules · doi:10.3390/biom16040567 · Cited by 1 · see citing works

Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs

Zhang, J., Cai, Y.-S., Ji, H., Ma, M., Zhang, J., Cheng, Z., Wang, K., Jiang, C., Zhuang, C., Hu, Y., et al. (2023) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2023.129468 · Cited by 1 · see citing works

In silico approach of bioactive molecule chitosan 501.1 kDa from snail shell as antioxidant and inhibitor of the keap1-nrf2 protein-protein interaction

Umarudin, U., Widyarti, S., Warsito, W., & Rahayu, S. (2023) · Pharmacy Education · doi:10.46542/pe.2023.234.510 · Cited by 1 · see citing works

Modulators of KEAP-1 Activity as Potential Therapies for the Treatment of Neurodegenerative Disorders

Blass, B. E. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00328 · Cited by 1 · see citing works

Design and Synthesis of Novel Small-Molecule Inhibitors of the Keap1-Nrf2 PPI

Sigtryggsson, S. B. (2019) · Uppsala University Publications (Uppsala University)

Harnessing the power of traditional Chinese medicine for targeted protein degradation

Wu, Z., Zhu, B., Shou, Y., & Guo, H. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-21816-3.00011-7

Omaveloxolone: a nuclear factor erythroid 2-related factor 2 activator for Friedreich’s ataxia

Zhao, Z., Wang, J., Lu, M., You, Q., & Jiang, Z. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-33885-4.00038-x

Disrupting E3 ubiquitin ligase protein–protein interactions in cancer: chemical modalities, mechanisms, and therapeutic opportunities

Kamel, E. M., Khadrawy, S. M., Ali, M. A. M., Ahmed, N. A., Yassin, N. Y. S., Alkhedhairi, S., Alkhayl, F. F. A., & Lamsabhi, A. M. (2026) · Biochemical Pharmacology · doi:10.1016/j.bcp.2026.117951

Discovery of a novel covalent allosteric site CYS434 in Keap1 and its ligand for the treatment of acute lung injury

Shi, Y., Tie, X., Tao, G., Jia, Y., Huang, Q., Lu, G., & Wu, Y. (2026) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2026.118716

A Keap1-Nrf2 protein-protein interaction inhibitor 4–95 ameliorates cognitive dysfunction by suppressing neuronal ferroptosis

Liu, R., Wei, M., Xu, L., Qu, Z., Yu, J.-Q., Liu, Y., Zhang, W.-N., Zhang, D., & Zhuang, C. (2026) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2026.110134

Development of potent BChE/Nrf2 modulators for Alzheimer's disease treatment via dual suppression of ferroptosis

Wang, Y., Sang, J., Li, H., Ren, X., Chen, C., Zheng, N., Xiao, H., Wei, Y., Xu, L., Jiang, R., et al. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.119093

Redox homeostasis and oxidative stress adaptation in cancer therapy resistance

Khojayeva, K., Khikhmetova, K., Maratzhan, M., & Aljofan, M. (2026) · Scientific Reviews · doi:10.1038/s44573-026-00015-z

BindingDB Entry 50023204: Discovery of β-amino acid substituted naphthalene sulfonamide derivatives as potent Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitors for ulcerative colitis management.

BindingDB (2026) · UC San Diego · doi:10.7270/q24t6q8p

BindingDB Entry 50011439: Design, Synthesis, and Structure-Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.

BindingDB (2022) · UC San Diego · doi:10.7270/q2vd7329

BindingDB Entry 50017940: TBA

BindingDB (2023) · UC San Diego · doi:10.7270/q2q52trd

BindingDB Entry 50020317: Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs.

BindingDB (2024) · UC San Diego · doi:10.7270/q2bv7n2r

BindingDB Entry 50014497: Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy.

BindingDB (2022) · UC San Diego · doi:10.7270/q2jh3r1f

BindingDB Entry 50001541: Discovery of a head-to-tail cyclic peptide as the Keap1-Nrf2 protein-protein interaction inhibitor with high cell potency.

BindingDB (2020) · UC San Diego · doi:10.7270/q2pk0jnt

BindingDB Entry 50016274: Structure-activity relationships of 1,4-bis(arylsulfonamido)-benzene or naphthalene-N,N'-diacetic acids with varying C2-substituents as inhibitors of Keap1-Nrf2 protein-protein interaction.

BindingDB (2023) · UC San Diego · doi:10.7270/q2f193rh

BindingDB Entry 50020171: Medicinal Chemistry Insights into the Development of Small-Molecule Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.

BindingDB (2024) · UC San Diego · doi:10.7270/q2sj1r16

BindingDB Entry 50018045: Natural Product-Inspired Targeted Protein Degraders: Advances and Perspectives.

BindingDB (2023) · UC San Diego · doi:10.7270/q2pv6qh4

BindingDB Entry 50018333: Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors.

BindingDB (2024) · UC San Diego · doi:10.7270/q2b85dbt

BindingDB Entry 50008207: Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity.

BindingDB (2021) · UC San Diego · doi:10.7270/q2cr5xq3

BindingDB Entry 50014015: Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.

BindingDB (2022) · UC San Diego · doi:10.7270/q23t9n1j

Rapid Identification of Keap1–Nrf2 Small-Molecule Inhibitors through Structure-Based Virtual Screening and Hit-Based Substructure Search

Zhuang, C., Narayanapillai, S. C., Zhang, W., Sham, Y. Y., & Xing, C. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm4017174 · Cited by 156 · see citing works

Emerging Screening Approaches in the Development of Nrf2–Keap1 Protein–Protein Interaction Inhibitors

Leung, C., Zhang, J.-T., Yang, G., Liu, H., Han, Q., & Ma, D. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20184445 · Cited by 55 · see citing works

Novel protein–protein interaction inhibitor of Nrf2–Keap1 discovered by structure-based virtual screening

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Updated Research and Applications of Small Molecule Inhibitors of Keap1-Nrf2 Protein-Protein Interaction: a Review

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