An inhibitor of Bcl-2 family proteins induces regression of solid tumours

Cell Death

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Distinct BH3 domains either sensitize or activate mitochondrial apoptosis, serving as prototype cancer therapeutics

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Activation of Apoptosis in Vivo by a Hydrocarbon-Stapled BH3 Helix

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Structural biology of the Bcl-2 family of proteins

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Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP

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The novel BH3 α-helix mimetic JY-1-106 induces apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein–protein interactions with Bak

Cao, X., Yap, J. L., Newell-Rogers, M. K., Peddaboina, C., Jiang, W., Papaconstantinou, H. T., Jupitor, D., Rai, A., Jung, K.-Y., Tubin, R. P., et al. (2013) · Molecular Cancer · doi:10.1186/1476-4598-12-42 · Cited by 87

Small molecule modulators of protein-protein interactions: selected case studies

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A BH3 Mimetic for Killing Cancer Cells

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Kinetin riboside preferentially induces apoptosis by modulating Bcl-2 family proteins and caspase-3 in cancer cells

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Consequences of the combined loss of BOK and BAK or BOK and BAX

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Modulating Protein–Protein Interactions with Small Molecules: The Importance of Binding Hotspots

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Inhibition of Rac GTPase signaling and downstream prosurvival Bcl-2 proteins as combination targeted therapy in MLL-AF9 leukemia

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Small molecules targeting protein–protein interactions for cancer therapy

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Plucking the high hanging fruit: A systematic approach for targeting protein–protein interactions

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Enzyme-cleavable polymeric micelles for the intracellular delivery of proapoptotic peptides

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The BH3 mimetic ABT-263 synergizes with the MEK1/2 inhibitor selumetinib/AZD6244 to promote BIM-dependent tumour cell death and inhibit acquired resistance

Sale, M. J., & Cook, S. J. (2013) · Biochemical Journal · doi:10.1042/bj20121212 · Cited by 58

Inflammation and survival pathways: Chronic lymphocytic leukemia as a model system

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Senolytic Targeting of Bcl-2 Anti-Apoptotic Family Increases Cell Death in Irradiated Sarcoma Cells

Lafontaine, J., Cardin, G. B., Malaquin, N., Boisvert, J.-S., Rodier, F., & Wong, P. (2021) · Cancers · doi:10.3390/cancers13030386 · Cited by 54

PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation

Anderson, G. R., Wardell, S. E., Cakir, M., Crawford, L., Leeds, J. C., Nussbaum, D. P., Shankar, P. S., Soderquist, R. S., Stein, E. M., Tingley, J. P., et al. (2016) · Science Translational Medicine · doi:10.1126/scitranslmed.aae0348 · Cited by 53

Targeting protein–protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies?

Cierpicki, T., & Grembecka, J. (2015) · Immunological Reviews · doi:10.1111/imr.12244 · Cited by 53

Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo

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MicroRNA-138 promotes acquired alkylator resistance in glioblastoma by targeting the Bcl-2-interacting mediator BIM

Stojcheva, N., Schechtmann, G., Sass, S., Roth, P., Florea, A.-M., Stefanski, A., Stühler, K., Wolter, M., Müller, N. S., Theis, F. J., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.7346 · Cited by 50

BH3 activation blocks Hdmx suppression of apoptosis and cooperates with Nutlin to induce cell death

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Androgen receptor ligand-binding domain interaction and nuclear receptor specificity of FXXLF and LXXLL motifs as determined by L/F swapping

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Helping the released guardian: Drug combinations for supporting the anticancer activity of HDM2 (MDM2) antagonists

Kocik, J., Machula, M., Wisniewska, A., Surmiak, E., Holak, T. A., & Skalniak, L. (2019) · Cancers · doi:10.3390/cancers11071014 · Cited by 46

BIM-mediated membrane insertion of the BAK pore domain is an essential requirement for apoptosis

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Rag1 immunodeficiency-induced early aging and senescence in zebrafish are dependent on chronic inflammation and oxidative stress

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Oncogenic RAS simultaneously protects against anti-EGFR antibody-dependent cellular cytotoxicity and EGFR signaling blockade

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Phosphorylation alters Bim‐mediated Mcl‐1 stabilization and priming

Conage‐Pough, J. E., & Boise, L. H. (2018) · The FEBS Journal · doi:10.1111/febs.14505 · Cited by 32

Destruction of tumor vasculature and abated tumor growth upon VEGF blockade is driven by proapoptotic protein Bim in endothelial cells

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BH3 Mimetics in Hematologic Malignancies

Klener, P., Sovilj, D., Renesova, N., & Andera, L. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms221810157 · Cited by 31

Regulation of HA14-1 mediated oxidative stress, toxic response, and autophagy by curcumin to enhance apoptotic activity in human embryonic kidney cells

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Apoptotic priming is defined by the dynamic exchange of Bcl-2 proteins between mitochondria and cytosol

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Therapeutics Targeting the Core Apoptotic Machinery

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Distinctive expression of bcl-2 factors in regulatory T cells determines a pharmacological target to induce immunological tolerance

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Structure–activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction

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PICKLUSTER: a protein-interface clustering and analysis plug-in for UCSF ChimeraX

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Identification of Repurposable Drugs and Adverse Drug Reactions for Various Courses of COVID-19 Based on Single-Cell RNA Sequencing Data

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Therapeutic development in targeting protein–protein interactions with synthetic topological mimetics

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Protein-Protein Interactions as Drug Targets

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Main methods and tools for peptide development based on protein-protein interactions (PPIs)

Baeza, J., Bedoya, M., Cruz, P., Ojeda, P., Adasme-Carreño, F., Cerda, O., & González, W. (2025) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2025.151623 · Cited by 8

PICKLUSTER: A protein-interface clustering and analysis plug-in for UCSF ChimeraX

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