The DOI matches its Crossref record; 52 of the 52 references it cites were found in a registry or an index.
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models
Abstract
Avoidance of apoptosis is critical for the development and sustained growth of tumours. The pro-survival protein myeloid cell leukemia 1 (MCL1) is overexpressed in many cancers, but the development of small molecules targeting this protein that are amenable for clinical testing has been challenging. Here we describe S63845, a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. Our mechanistic studies demonstrate that S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. In vivo, S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Moreover, MCL1 inhibition, either alone or in combination with other anti-cancer drugs, proved effective against several solid cancer-derived cell lines. These results point towards MCL1 as a target for the treatment of a wide range of tumours.
Overview
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
In the citing paper
“Prior studies have demonstrated that sensitivity of cancer cells to MCL-1 inhibition is inversely related to BCL-XL expression level and the capacity for BCL-XL to neutralize pro-apoptotic BH3 proteins such as BIM60,61.”
From LKB1 regulates JNK-dependent stress signaling and apoptotic dependency of KRAS-mutant lung cancers (2025) · cites this paper as [60]
In the citing paper
“Conversely, the BCL2 inhibitor venetoclax is currently available for the treatment of CLL patients who fail to obtain clinical benefit from conventional therapies [1046], and several other molecules with a similar mechanism of action are currently in clinical development [118] (source https://clinicaltrials.gov/).”
From Molecular mechanisms of cell death: recommendations of the nomenclature committee on cell death 2018. (2018) · cites this paper as [118]
Citations
Cites
Hallmarks of Cancer: The Next Generation
Hanahan, D., & Weinberg, R. A. (2011) · Cell · doi:10.1016/j.cell.2011.02.013 · Cited by 66,590
Kabsch, W. (2010) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444909047337 · Cited by 16,463
Refinement of Macromolecular Structures by the Maximum-Likelihood Method
Murshudov, G. N., Vagin, A. A., & Dodson, E. J. (1997) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444996012255 · Cited by 14,796
MOLREP : an Automated Program for Molecular Replacement
Vagin, A. A., & Teplyakov, A. (1997) · Journal of Applied Crystallography · doi:10.1107/s0021889897006766 · Cited by 4,756
The landscape of somatic copy-number alteration across human cancers
Beroukhim, R., Mermel, C. H., Porter, D., Wei, G., Raychaudhuri, S., Donovan, J., Barretina, J., Boehm, J. S., Dobson, J., Urashima, M., et al. (2010) · Nature · doi:10.1038/nature08822 · Cited by 4,017
An inhibitor of Bcl-2 family proteins induces regression of solid tumours
Oltersdorf, T., Elmore, S. W., Shoemaker, A. R., Armstrong, R. C., Augeri, D. J., Belli, B., Bruncko, M., Deckwerth, T. L., Dinges, J., Hajduk, P. J., et al. (2005) · Nature · doi:10.1038/nature03579 · Cited by 3,407
Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy
Czabotar, P. E., Lessene, G., Strasser, A., & Adams, J. M. (2014) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3722 · Cited by 3,219
Self-citationABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets
Souers, A. J., Leverson, J. D., Boghaert, E. R., Ackler, S. L., Catron, N. D., Chen, J., Dayton, B. D., Ding, H., Enschede, S. H., Fairbrother, W. J., et al. (2013) · Nature Medicine · doi:10.1038/nm.3048 · Cited by 3,058
Self-citationTargeting BCL2 with Venetoclax in Relapsed Chronic Lymphocytic Leukemia
Roberts, A. W., Davids, M. S., Pagel, J. M., Kahl, B. S., Puvvada, S. D., Gerecitano, J. F., Kipps, T. J., Anderson, M. A., Brown, J. R., Gressick, L. A., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1513257 · Cited by 1,930
Self-citationChen, L., Willis, S. N., Wei, A., Smith, B. J., Fletcher, J. I., Hinds, M. G., Colman, P. M., Day, C. L., Adams, J. M., & Huang, D. C. S. (2005) · Molecular Cell · doi:10.1016/j.molcel.2004.12.030 · Cited by 1,816
Self-citation
Cited by
Sorted by citations
Items 501–600 of 1,001
Discovery of Mcl-1 inhibitors from integrated high throughput and virtual screening
Mady, A. S. A., Liao, C., Bajwa, N., Kump, K. J., Abulwerdi, F. A., Lev, K. L., Miao, L., Grigsby, S. M., Perdih, A., Stuckey, J. A., et al. (2018) · Scientific Reports · doi:10.1038/s41598-018-27899-9 · Cited by 19
Arulananda, S., Lee, E. F., Fairlie, W. D., & John, T. (2020) · Expert Review of Anticancer Therapy · doi:10.1080/14737140.2021.1856660 · Cited by 19
Jurić, V., Hudson, L., Fay, J., Richards, C. E., Jahns, H., Verreault, M., Bielle, F., Idbaïh, A., Lamfers, M. L. M., Hopkins, A. M., et al. (2021) · Cell Death and Disease · doi:10.1038/s41419-021-04050-7 · Cited by 19
In vivo inducible reverse genetics in patients’ tumors to identify individual therapeutic targets
Carlet, M., Völse, K., Vergalli, J., Becker, M., Herold, T., Arner, A., Senft, D., Jurinović, V., Liu, W., Gao, Y., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-25963-z · Cited by 19
Peng, Z., Gillissen, B. F., Richter, A., Sinnberg, T. W., Schlaak, M. S., & Eberle, J. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24054961 · Cited by 19
Tarr, J. C., Salovich, J. M., Aichinger, M., Jeon, K., Veerasamy, N., Sensintaffar, J., Arnhof, H., Samwer, M., Christov, P. P., Kim, K., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01188 · Cited by 19
Guo, L., Lin, P., Xiong, H., Tu, S., & Chen, G. (2018) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2018.01.001 · Cited by 20
Rationally derived drug combinations with the novel Mcl-1 inhibitor EU-5346 in breast cancer
Vallet, S., Fan, F., Malvestiti, S., Pecherstorfer, M., Sattler, M., Schneeweiß, A., Schulze‐Bergkamen, H., Opferman, J. T., Cardone, M. H., Jäger, D., et al. (2018) · Breast Cancer Research and Treatment · doi:10.1007/s10549-018-5022-5 · Cited by 19
Suleiman, M. R., Wang, H., Huang, D., Wang, H., Joseph, J., Huang, T., Zhang, F., Wang, J., & Cheng, M. (2020) · Journal of Biomolecular Structure and Dynamics · doi:10.1080/07391102.2020.1749132 · Cited by 19
Self-citationLi, Y., Fan, W., Gong, Q., Tian, J., Zhou, M., Li, Q., Uwituze, L. B., Zhang, Z., Hong, R., & Wang, R. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00690 · Cited by 19
Jayappa, K. D., Gordon, V. L., Morris, C. G., Wilson, B., Shetty, B. D., Cios, K. J., Arora, P. C., Isaac, K. M., Saha, S., Bender, T. P., et al. (2021) · Blood Advances · doi:10.1182/bloodadvances.2020003944 · Cited by 19
Sulkshane, P., & Teni, T. R. (2022) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2022.00083 · Cited by 19
Rationale for a Combination Therapy Consisting of MCL1- and MEK-Inhibitors in Acute Myeloid Leukemia
Seipel, K., Schmitter, K., Bacher, U., & Pabst, T. (2019) · Cancers · doi:10.3390/cancers11111779 · Cited by 19
Key residues in the VDAC2-BAK complex can be targeted to modulate apoptosis
Yuan, Z., van Delft, M. F., Li, X., Sumardy, F., Smith, B. J., Huang, D. C. S., Lessène, G., Khakam, Y., Jin, R., He, S., et al. (2024) · PLoS Biology · doi:10.1371/journal.pbio.3002617 · Cited by 18
Self-citationRelative importance of the anti-apoptotic versus apoptosis-unrelated functions of MCL-1 in vivo
Brinkmann, K., McArthur, K., Malelang, S., Gibson, L., Tee, A., Doomun, S. N. E., Rowe, C. L., Arandjelovic, P., Marchingo, J. M., D’Silva, D. B., et al. (2025) · Science · doi:10.1126/science.adw1836 · Cited by 18
Self-citationRNA Pol II inhibition activates cell death independently from the loss of transcription
Harper, N. W., Birdsall, G. A., Honeywell, M. E., Ward, K. M., Pai, A. A., & Lee, M. J. (2025) · Cell · doi:10.1016/j.cell.2025.07.034 · Cited by 18
Wang, C. Y., Guo, S., Croft, A. J., Yan, X. G., Jin, L., Zhang, X. D., & Jiang, C. C. (2017) · Molecular Carcinogenesis · doi:10.1002/mc.22755 · Cited by 18
Discovery, development and application of drugs targeting BCL-2 pro-survival proteins in cancer
Lee, E. F., & Fairlie, W. D. (2021) · Biochemical Society Transactions · doi:10.1042/bst20210749 · Cited by 18
Klanova, M., Kazantsev, D., Pokorna, E., Zikmund, T., Karolová, J., Behounek, M., Renešová, N., Sovilj, D., Kelemen, C. D., Helman, K., et al. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-0511 · Cited by 18
Super-Resolution Microscopy to Study Interorganelle Contact Sites
Nieto‐Garai, J. A., Olazar‐Intxausti, J., Anso, I., Lorizate, M., Terrones, O., & Contreras, F. ‐. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms232315354 · Cited by 20
Adhikary, U., Paulo, J. A., Godes, M., Roychoudhury, S., Prew, M. S., Ben‐Nun, Y., Yu, E. W., Budhraja, A., Opferman, J. T., Chowdhury, D., et al. (2023) · Cell Reports · doi:10.1016/j.celrep.2023.113176 · Cited by 19
Arnett, E., Pahari, S., Wager, C. M. L., Hernandez, E., Bonifacio, J. R., Lumbreras, M., Renshaw, C. W., Montoya, M., Opferman, J., & Schlesinger, L. S. (2023) · Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · doi:10.1016/j.biopha.2023.115738 · Cited by 20
Role of apoptosis in the development of autosomal dominant polycystic kidney disease (ADPKD)
Peintner, L., & Borner, C. (2017) · Cell and Tissue Research · doi:10.1007/s00441-017-2628-6 · Cited by 18
Riz, I., & Hawley, R. G. (2017) · Oncoscience · doi:10.18632/oncoscience.356 · Cited by 18
Grundy, M. A., Seedhouse, C., Jones, T., Elmi, L., Hall, M., Graham, A., Russell, N. H., & Pallis, M. (2018) · PLoS ONE · doi:10.1371/journal.pone.0190682 · Cited by 18
BAK/BAX-Mediated Apoptosis Is a Myc-Induced Roadblock to Reprogramming
Kim, E. J. Y., Änkö, M., Flensberg, C., Majewski, I. J., Geng, F., Firas, J., Huang, D. C. S., van Delft, M. F., & Heath, J. K. (2018) · Stem Cell Reports · doi:10.1016/j.stemcr.2017.12.019 · Cited by 19
Self-citationSynergistic antitumor effects of 9.2.27-PE38KDEL and ABT-737 in primary and metastatic brain tumors
Yu, X., Dobrikov, M. I., Keir, S. T., Gromeier, M., Pastan, I. H., Reisfeld, R. A., Bigner, D. D., & Chandramohan, V. (2019) · PLoS ONE · doi:10.1371/journal.pone.0210608 · Cited by 18
Diepstraten, S. T., Chang, C. W. T., Tai, L., Gong, J., Lan, P., Dowell, A. C., Taylor, G. S., Strasser, A., & Kelly, G. L. (2020) · Blood Advances · doi:10.1182/bloodadvances.2019000541 · Cited by 18
Self-citationDing, X., Zhang, Y., Huang, T., Xu, G., Peng, C., Chen, G., Kong, B., Frieß, H., Shen, S., Lv, Y., et al. (2019) · PubMed Central · Cited by 18
Interdiction at a protein-protein interface: MCL-1 inhibitors for oncology
Li, K. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127717 · Cited by 18
The role of post-translational modifications in the regulation of MCL1
Li, S., Guo, W., & Wu, H. (2021) · Cellular Signalling · doi:10.1016/j.cellsig.2021.109933 · Cited by 19
Drimane Derivatives as the First Examples of Covalent BH3 Mimetics that Target MCL‐1
Daressy, F., Malard, F., Séguy, L., Guérineau, V., Apel, C., Dumontet, V., Robert, A., Groo, A., Litaudon, M., Bignon, J. S., et al. (2021) · ChemMedChem · doi:10.1002/cmdc.202100011 · Cited by 18
Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins
Pal, P., Zhang, P., Poddar, S. K., & Zheng, G. (2022) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2022.2116311 · Cited by 18
Overcoming Steroid Resistance in T Cell Acute Lymphoblastic Leukemia
Goossens, S., & Vlierberghe, P. V. (2016) · PLoS Medicine · doi:10.1371/journal.pmed.1002208 · Cited by 18
Targeting Mcl-1 inhibits survival and self-renewal of hepatocellular cancer stem-like cells
Zhang, H., Li, G., Chen, G., Zhang, Y., Pan, J., Tang, H., Li, J., Guo, W., & Zhang, S. (2018) · Clinics and Research in Hepatology and Gastroenterology · doi:10.1016/j.clinre.2018.11.004 · Cited by 18
Targeting Cancer's Achilles’ Heel: Role of BCL-2 Inhibitors in Cellular Senescence and Apoptosis
Anantram, A., & Degani, M. S. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2018-0366 · Cited by 18
Structural basis of BAK sequestration by MCL-1 in apoptosis
Srivastava, S., Sekar, G., Ojoawo, A. M., Aggarwal, A., Ferreira, E., Uchikawa, E., Yang, M., Grace, C. R., Dey, R., Lin, Y.-L., et al. (2025) · Molecular Cell · doi:10.1016/j.molcel.2025.03.013 · Cited by 17
Myeloid cell leukemin-1 inhibitors: a growing arsenal for cancer therapy
Zhu, P., Yu, Z.-Z., You, Q., & Jiang, Z. (2020) · Drug Discovery Today · doi:10.1016/j.drudis.2020.07.021 · Cited by 19
Exploiting Protein Translation Dependence in Multiple Myeloma with Omacetaxine-Based Therapy
Walker, Z. J., Idler, B. M., Davis, L. N., Stevens, B. M., VanWyngarden, M. J., Ohlstrom, D. J., Bearrows, S. C., Hammes, A., Smith, C. A., Jordan, C. T., et al. (2020) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-20-2246 · Cited by 17
Jayappa, K. D., Tran, B., Gordon, V. L., Morris, C. G., Saha, S., Farrington, C. C., O’Connor, C. M., Zawacki, K. P., Isaac, K. M., KESTER, M. A., et al. (2023) · Journal of Clinical Investigation · doi:10.1172/jci155938 · Cited by 17
Zhang, H., Zhang, J., Luan, S., Liu, Z., Li, X., Liu, B., & Yuan, Y. (2023) · International Journal of Biological Sciences · doi:10.7150/ijbs.85753 · Cited by 17
Kaplan, Ö., Gök, M. K., Pekmez, M., Tayhan, S. E., Özgümüş, S., Gökçe, İ., & Arda, N. (2024) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2024.105565 · Cited by 17
Dolníková, A., Kazantsev, D., Klánová, M., Pokorna, E., Sovilj, D., Kelemen, C. D., Tušková, L., Hoferkova, E., Mráz, M., Helman, K., et al. (2024) · Blood Advances · doi:10.1182/bloodadvances.2024012906 · Cited by 17
Engineering anti-BCMA CAR T cells for enhancing myeloma killing efficacy via apoptosis regulation
Kimman, T., Cuenca, M., Tieland, R. G., Rockx-Brouwer, D., Janssen, J., Motais, B., Slomp, A., Pleijte, C., Heijhuurs, S., Meringa, A. D., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-59818-8 · Cited by 17
Design, synthesis and biological evaluation of tyrosine derivatives as Mcl-1 inhibitors
Liu, L., Liu, R., Yang, X., Hou, X., & Fang, H. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112142 · Cited by 17
SUMOylation of MCL1 protein enhances its stability by regulating the ubiquitin-proteasome pathway
Li, S., Wang, J., Hu, G., Aman, S., Li, B., Li, Y., Xia, K., Yang, Y., Ahmad, B., Wang, M., et al. (2020) · Cellular Signalling · doi:10.1016/j.cellsig.2020.109686 · Cited by 17
Valiulienė, G., Vitkevičienė, A., Skliutė, G., Borutinskaite, V. V., & Navakauskienė, R. (2021) · Molecules · doi:10.3390/molecules26082303 · Cited by 17
Malyukova, A., Ujvári, D., Yektaei‐Karin, E., Zovko, A., Madapura, H. S., Keszei, M., Nagy, N., Lotfi, K., Björn, N., Wallvik, J., et al. (2021) · Cell Death and Disease · doi:10.1038/s41419-021-04154-0 · Cited by 18
Specific Targeting of Antiapoptotic Bcl-2 Proteins as a Radiosensitizing Approach in Solid Tumors
Sobol, B., Nieto, O. A., Eberlein, E. L., Scherr, A., Ismail, L., Kessler, A., Nader, L., Schwab, M., Hoffmeister‐Wittmann, P., Schmitt, N., et al. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23147850 · Cited by 17
Daressy, F., Séguy, L., Favre, L., Corvaisier, S., Apel, C., Groo, A., Litaudon, M., Dumontet, V., Malzert‐Fréon, A., Desrat, S., et al. (2022) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2022.113546 · Cited by 17
Yan, G., Luna, A., Wang, H., Bozorgui, B., Li, X., Sanchez, M., Dereli, Z., Kahraman, N., Kara, G., Chen, X., et al. (2020) · Cell Reports · doi:10.1016/j.celrep.2022.111304 · Cited by 18
Kröhnke pyridines: Rapid and facile access to Mcl-1 inhibitors
Conlon, I. L., Eker, D. V., Abdelmalak, S., Murphy, W. A., Bashir, H., Sun, M. A., Chauhan, J., Varney, K. M., Godoy‐Ruiz, R., Wilder, P. T., et al. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.03.050 · Cited by 17
Counting on Death – Quantitative aspects of Bcl‐2 family regulation
Hantusch, A., Rehm, M., & Brunner, T. (2018) · FEBS Journal · doi:10.1111/febs.14516 · Cited by 17
Structure-guided design of pyridoclax derivatives based on Noxa / Mcl-1 interaction mode
Hedir, S., Giorgi, M. D., Fogha, J., Pascale, M. D., Weiswald, L., Brotin, É., Marekha, B., Denoyelle, C., Denis, C., Suzanne, P., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.10.003 · Cited by 20
Venetoclax, bortezomib and S63845, an MCL1 inhibitor, in multiple myeloma
Wong, K. Y., & Chim, C. S. (2020) · Journal of Pharmacy and Pharmacology · doi:10.1111/jphp.13240 · Cited by 17
Naghdi, S., Mishra, P., Roy, S. S., Weaver, D., Walter, L., Davies, E., Antony, A. N., Lin, X., Moehren, G., Feitelson, M. A., et al. (2025) · Nature Communications · doi:10.1038/s41467-025-56898-4 · Cited by 17
Mcl‐1 targeting strategies unlock the proapoptotic potential of TRAIL in melanoma cells
Sarif, Z., Tolksdorf, B., Fechner, H., & Eberle, J. (2020) · Molecular Carcinogenesis · doi:10.1002/mc.23253 · Cited by 16
Mucci, S., Isaja, L., Rodríguez-Varela, M. S., Ferriol-Laffouillere, S. L., Marazita, M. C., Videla-Richardson, G. A., Sevlever, G. E., Scassa, M. É., & Romorini, L. (2022) · Scientific Reports · doi:10.1038/s41598-022-23650-7 · Cited by 17
Michalski, M., Bauer, M., Walz, F., Tümen, D., Heumann, P., Stöckert, P., Gunckel, M., Kunst, C., Kandulski, A., Schmid, S. A., et al. (2023) · Biomedicines · doi:10.3390/biomedicines11061666 · Cited by 20
FBXW7 and human tumors: mechanisms of drug resistance and potential therapeutic strategies
Wang, W., Jiang, K., Liu, X., Li, J., Zhou, W., Wang, C., Cui, J., & Liang, T. (2023) · Frontiers in Pharmacology · doi:10.3389/fphar.2023.1278056 · Cited by 16
Recent therapeutic advances in chronic lymphocytic leukemia
Bose, P., & Gandhi, V. V. (2017) · F1000Research · doi:10.12688/f1000research.11618.1 · Cited by 16
Jiao, Y., Davis, J. E., Rautela, J., Carrington, E. M., Ludford‐Menting, M., Goh, W., Delconte, R. B., Souza-Fonseca-Guimarães, F., Koldej, R. M., Gray, D. H. D., et al. (2018) · Cell Death and Differentiation · doi:10.1038/s41418-018-0228-y · Cited by 16
Self-citationConlon, I. L., Drennen, B., Lanning, M. E., Hughes, S., Rothhaas, R., Wilder, P. T., MacKerell, A. D., & Fletcher, S. (2020) · ChemMedChem · doi:10.1002/cmdc.202000278 · Cited by 16
Mallick, D. J., & Eastman, A. R. (2020) · Cancers · doi:10.3390/cancers12082298 · Cited by 16
Query-guided protein–protein interaction inhibitor discovery
Celis, S., Hóbor, F., James, T., Bartlett, G. J., Ibarra, A. Á., Shoemark, D. K., Hegedüs, Z., Hetherington, K., Woolfson, D. N., Sessions, R. B., et al. (2021) · Chemical Science · doi:10.1039/d1sc00023c · Cited by 17
Importance of Bcl-2-family proteins in murine hematopoietic progenitor and early B cells
Kurschat, C., Metz, A., Kirschnek, S., & Häcker, G. A. (2021) · Cell Death and Disease · doi:10.1038/s41419-021-04079-8 · Cited by 17
Huang, A. S., Chin, H. S., Reljić, B., Djajawi, T. M., Tan, I. K. L., Gong, J., Stroud, D. A., Huang, D. C. S., van Delft, M. F., & Dewson, G. (2022) · Cell Death and Differentiation · doi:10.1038/s41418-022-01067-z · Cited by 17
Self-citationLuan, S., Ge, Q. P., Chen, Y., Dai, M., Yang, J., Li, K., Liu, D., & Zhao, L. (2017) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2017.03.028 · Cited by 16
Preferential targeting of MCL-1 by a hydrocarbon-stapled BIM BH3 peptide
Hadji, A., Schmitt, G. K., Schnorenberg, M. R., Roach, L. E., Hickey, C. M., Leak, L. B., Tirrell, M., & LaBelle, J. L. (2019) · Oncotarget · doi:10.18632/oncotarget.27262 · Cited by 16
Targeting the apoptotic Mcl-1-PUMA interface with a dual-acting compound
Liu, J., Tian, Z., Zhou, N., Liu, X., Liao, C., Lei, B., Li, J., Zhang, S., & Chen, H. (2017) · Oncotarget · doi:10.18632/oncotarget.17294 · Cited by 15
Cell-penetrating Alphabody protein scaffolds for intracellular drug targeting
Pannecoucke, E., Trimpont, M. V., Desmet, J., Pieters, T., Reunes, L., Demoen, L., Vuylsteke, M., Loverix, S., Vandenbroucke, K., Alard, P., et al. (2021) · Science Advances · doi:10.1126/sciadv.abe1682 · Cited by 15
MEK and MCL-1 sequential inhibition synergize to enhance rhabdomyosarcoma treatment
Alcon, C., Martín, F., Prada, E., Mora, J., Soriano, A., Guillén, G., Gallego, S., Roma, J. M., Samitier, J., Villanueva, A., et al. (2022) · Cell Death Discovery · doi:10.1038/s41420-022-00959-w · Cited by 18
Vera, M. B., Morris-Hanon, O., Nogueiras, G. I., Ripari, L. B., Esquivel, M. I., Perez-Castro, C., Romorini, L., Sevlever, G. E., Scassa, M. É., & Videla-Richardson, G. A. (2022) · Scientific Reports · doi:10.1038/s41598-022-20910-4 · Cited by 16
Genetic mutations affecting mitochondrial function in cancer drug resistance
Lee, C., Park, S., & Yoon, S. K. (2023) · Genes & Genomics · doi:10.1007/s13258-022-01359-1 · Cited by 15
Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1
Demin, S., Peschiulli, A., Velter, A. I., Vos, A. M., Boeck, B. D., Miller, B., Rombouts, F. J. R., Reuillon, T. D., Lento, W. E., Blanco, M. D., et al. (2023) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.3c00141 · Cited by 15
Non-genetic mechanisms of drug resistance in acute leukemias
Calderon, A., Han, C., Karma, S., & Wang, E. (2023) · Trends in cancer · doi:10.1016/j.trecan.2023.09.003 · Cited by 17
Apoptosis Inhibitor 5: A Multifaceted Regulator of Cell Fate
Abbas, H., Derkaoui, D. K., Jeammet, L., Adicéam, E., Tiollier, J., Sicard, H., Braun, T., & Poyet, J. (2024) · Biomolecules · doi:10.3390/biom14010136 · Cited by 16
Suo, S., Sun, S., Nguyen, L. X. T., Qian, J., Li, F., Zhao, D., Yu, W., Lou, Y., Zhu, H., Tong, H., et al. (2024) · Med · doi:10.1016/j.medj.2024.07.018 · Cited by 15
Yang, X., Mao, X., Ding, X., Guan, F., Jia, Y., Luo, L., Li, B., Tan, H., & Cao, C. (2018) · Cell Biology and Toxicology · doi:10.1007/s10565-018-9424-2 · Cited by 15
Uchihara, Y., Komori, R., Tago, K., Tamura, H., & Funakoshi‐Tago, M. (2019) · Biochemical Pharmacology · doi:10.1016/j.bcp.2019.113666 · Cited by 15
Enhancing venetoclax activity in hematological malignancies
Satta, T., & Grant, S. (2020) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2020.1789588 · Cited by 15
PROXIMA-1 beamline for macromolecular crystallography measurements at Synchrotron SOLEIL
Chavas, L. M. G., Gourhant, P., Guimarães, B. G., Isabet, T., Legrand, P., Lener, R., Montaville, P., Sirigu, S., & Thompson, A. (2021) · Journal of Synchrotron Radiation · doi:10.1107/s1600577521002605 · Cited by 15
He, S., Zimmerman, M. W., Layden, H. M., Berezovskaya, A., Etchin, J., Martel, M. W., Thurston, G., Jing, C., van Rooijen, E., Kaufman, C. K., et al. (2021) · Oncogene · doi:10.1038/s41388-021-01926-y · Cited by 15
Kim, S., Park, H.-S., & Oh, B. (2022) · Computational and Structural Biotechnology Journal · doi:10.1016/j.csbj.2022.06.021 · Cited by 15
Small molecule SJ572946 activates BAK to initiate apoptosis
Sekar, G., Singh, G., Qin, X., Guibao, C. D., Schwam, B., Inde, Z., Grace, C. R., Zhang, W., Slavish, P. J., Lin, W., et al. (2022) · iScience · doi:10.1016/j.isci.2022.105064 · Cited by 15
Aid, Z., Robert, E., Lopez, C. K., Bourgoin, M., Boudia, F., Mene, M. L., Rivière, J., Baille, M., Benbarche, S., Renou, L., et al. (2022) · Leukemia · doi:10.1038/s41375-022-01800-0 · Cited by 15
Synthetic lethality of drug-induced polyploidy and BCL-2 inhibition in lymphoma
Portelinha, A., Ferreira, M. D. S., Erazo, T., Jiang, M., Asgari, Z., de Stanchina, E., Younes, A., & Wendel, H. (2023) · Nature Communications · doi:10.1038/s41467-023-37216-2 · Cited by 15
Mcl-1 Protein and Viral Infections: A Narrative Review
Wyżewski, Z., Stępkowska, J., Kobylińska, A. M., Mielcarska, A., & Mielcarska, M. B. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25021138 · Cited by 14
Mghwary, A. E.-S., Hassan, R. A., Halim, P. A., & Abdelhameid, M. K. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107985 · Cited by 14
Mcl-1 inhibitor suppresses tumor growth of esophageal squamous cell carcinoma in a mouse model
Lin, J., Fu, D., Dai, Y., Lin, J., & Xu, T. (2017) · Oncotarget · doi:10.18632/oncotarget.18772 · Cited by 14
Procacci, P. (2018) · Journal of Chemical Theory and Computation · doi:10.1021/acs.jctc.8b00305 · Cited by 14
Reinhart, R., & Kaufmann, T. (2018) · Cell Death and Disease · doi:10.1038/s41419-018-0754-z · Cited by 14
Zou, J., Jones, R. J., Wang, H., Kuiatse, I., Shirazi, F., Manasanch, E. E., Lee, H. C., Sullivan, R., Fung, L. M., Richard, N., et al. (2020) · Journal of Molecular Medicine · doi:10.1007/s00109-020-01943-6 · Cited by 14
Morande, P. E., Yan, X., Sepúlveda-Yáñez, J., Seija, N., Márquez, M. E., Sotelo, N. S., Abreu, C., Crispo, M., Fernández-Graña, G., Rego, N., et al. (2021) · Blood · doi:10.1182/blood.2020008654 · Cited by 14
Lapidot, M., Case, A. E., Weisberg, E., Meng, C., Walker, S. R., Garg, S., Wei Min, N. I., Podar, K., Hung, Y. P., Carrasco, R. D., et al. (2021) · British Journal of Cancer · doi:10.1038/s41416-021-01441-7 · Cited by 15
Understanding the Species Selectivity of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors
Zhao, B., Arnold, A. L., Coronel, M. A., Lee, J. H., Lee, T., Olejniczak, E. T., & Fesik, S. W. (2018) · Biochemistry · doi:10.1021/acs.biochem.8b00626 · Cited by 14
The Discovery of Cryptic Pockets Increases the Druggability of “Undruggable” Proteins
Mou, M., Yang, W., Huang, G., Yang, X., Zhang, X. L., Kandegama, W., Ashby, C. R., Hao, G., & Gao, Y. (2025) · Medicinal Research Reviews · doi:10.1002/med.70001 · Cited by 14
Kamachi, K., Ureshino, H., Watanabe, T., Yoshida‐Sakai, N., Fukuda‐Kurahashi, Y., Kawasoe, K., Hoshiko, T., Yamamoto, Y., Kurahashi, Y., & Kimura, S. H. (2023) · Cancer Research Communications · doi:10.1158/2767-9764.crc-22-0259 · Cited by 13
Tiedt, R., King, F. J., Stamm, C., Niederst, M. J., Delach, S. M., Zumstein-Mecker, S., Meltzer, J., Mulford, I. J., Labrot, E., Engstler, B. S., et al. (2023) · Cell Reports · doi:10.1016/j.celrep.2023.112297 · Cited by 13
Perurena, N., Lock, R., Davis, R. A., Raghavan, S., Pilla, N. F., Ng, R. W. S., Loi, P., Guild, C. J., Miller, A. L., Sicińska, E., et al. (2023) · Cell Reports Medicine · doi:10.1016/j.xcrm.2023.101007 · Cited by 13
Metadata
- Authors
- Kotschy, A., Szlavik, Z., Murray, J., Davidson, J., Maragno, A. L., Le Toumelin-Braizat, G., Chanrion, M., Kelly, G. L., Gong, J.-N., Moujalled, D. M., Bruno, A., Csekei, M., Paczal, A., Szabo, Z. B., Sipos, S., Radics, G., Proszenyak, A., Balint, B., Ondi, L., Blasko, G., Robertson, A., Surgenor, A., Dokurno, P., Chen, I., Matassova, N., Smith, J., Pedder, C., Graham, C., Studeny, A., Lysiak-Auvity, G., Girard, A.-M., Gravé, F., Segal, D., Riffkin, C. D., Pomilio, G., Galbraith, L. C. A., Aubrey, B. J., Brennan, M. S., Herold, M. J., Chang, C., Guasconi, G., Cauquil, N., Melchiore, F., Guigal-Stephan, N., Lockhart, B., Colland, F., Hickman, J. A., Roberts, A. W., Huang, D. C. S., Wei, A. H., Strasser, A., Lessene, G., & Geneste, O.
- Affiliations
- Vernalis (R&D) Limited (United Kingdom) (GB)
- Institut de Recherches Internationales Servier (France) (FR)
- The University of Melbourne (AU)
- Monash University (AU)
- The Royal Melbourne Hospital (AU)
- The Alfred Hospital (AU)
- Corresponding author
- Geneste, Olivier
- ORCID
- Kotschy, András
- Murray, James
- Davidson, James
- Kelly, Gemma L.
- Moujalled, Donia M.
- Surgenor, Allan
- Dokurno, Pawel
- Chen, Ijen
- Matassova, Natalia
- Graham, Christopher
- Girard, Anne-Marie
- Segal, David
- Riffkin, Chris D.
- Galbraith, Laura C. A.
- Aubrey, Brandon J.
- Brennan, Margs S.
- Herold, Marco J.
- Chang, Catherine
- Melchiore, Fabien
- Colland, Frédéric
- Hickman, John A.
- Roberts, Andrew W.
- Huang, David C. S.
- Wei, Andrew H.
- Strasser, Andreas
- Venue
- Nature
- Published
- 2016-10
- Volume
- 538
- Issue
- 7626
- Pages
- 477-482
- ISSN
- 0028-0836 (ISSN-L)
- 1476-4687
- OpenAlex
- W2534349779
- Semantic Scholar
- 804d41f048a7386a3e6b3fcd1589511de3fabcd4
- Cited by
- 1,047
- References
- 52
- Citations by year
- 2026: 63 · 2025: 87 · 2024: 75 · 2023: 100 · 2022: 99 · 2021: 133 · 2020: 152 · 2019: 123 · 2018: 120 · 2017: 83 · 2016: 8
- FWCI
- 48.12
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature (publishedVersion)
- PubMed (publishedVersion)
- RePEc: Research Papers in Economics (submittedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cell death mechanisms and regulation
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Health Sciences › Medicine › Hematology › Acute Myeloid Leukemia Research
- Keywords
- S63845, BH3-binding groove, apoptosis, mitochondrial apoptosis, multiple myeloma, leukemia, lymphoma, solid tumors, antitumour activity, drug safety, combination therapy
- MeSH terms
- Animals, Antineoplastic Agents, Female, Humans, Leukemia, Lymphoma, Male, Models, Biological, Models, Molecular, Multiple Myeloma, Neoplasms, Pyrimidines, Thiophenes, Apoptosis, Xenograft Model Antitumor Assays, Cell Line, Tumor, bcl-2 Homologous Antagonist-Killer Protein, bcl-2-Associated X Protein, Mice, Myeloid Cell Leukemia Sequence 1 Protein
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review