Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP)

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 · see citing works

Smac, a Mitochondrial Protein that Promotes Cytochrome c–Dependent Caspase Activation by Eliminating IAP Inhibition

Du, C., Fang, M., Li, Y., Li, L., & Wang, X. (2000) · Cell · doi:10.1016/s0092-8674(00)00008-8 · Cited by 3,513 · see citing works

Improved protein–ligand docking using GOLD

Verdonk, M. L., Cole, J. C., Hartshorn, M. J., Murray, C. W., & Taylor, R. D. (2003) · Proteins Structure Function and Bioinformatics · doi:10.1002/prot.10465 · Cited by 3,073 · see citing works

Advances in methods and algorithms in a modern quantum chemistry program package

Shao, Y., Füsti-Molnár, L., Jung, Y., Kußmann, J., Ochsenfeld, C., Brown, S. T., Gilbert, A. T. B., Slipchenko, L. V., Levchenko, S. V., O'Neill, D. P., et al. (2006) · Physical Chemistry Chemical Physics · doi:10.1039/b517914a · Cited by 2,805 · see citing works

IAP family proteins---suppressors of apoptosisPreprint

Deveraux, Q. L., & Reed, J. C. (1999) · Genes & Development · doi:10.1101/gad.13.3.239 · Cited by 2,535 · see citing works

Ligand efficiency: a useful metric for lead selection

Hopkins, A. L., Groom, C. R., & Alex, A. (2004) · Drug Discovery Today · doi:10.1016/s1359-6446(04)03069-7 · Cited by 1,895 · see citing works

Molecular recognition of receptor sites using a genetic algorithm with a description of desolvation

Jones, G., Willett, P., & Glen, R. C. (1995) · Journal of Molecular Biology · doi:10.1016/s0022-2836(95)80037-9 · Cited by 1,548 · see citing works

Targeting IAP proteins for therapeutic intervention in cancer

Fulda, S., & Vucic, D. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3627 · Cited by 837 · see citing works

Motifs for molecular recognition exploiting hydrophobic enclosure in protein–ligand binding

Young, T. K., Abel, R., Kim, B., Berne, B. J., & Friesner, R. A. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0610202104 · Cited by 697 · see citing works

IAPs, RINGs and ubiquitylation

Vaux, D. L., & Silke, J. (2005) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm1621 · Cited by 611 · see citing works

Autocrine TNFα Signaling Renders Human Cancer Cells Susceptible to Smac-Mimetic-Induced Apoptosis

Petersen, S. L., Wang, L., Yalcin-Chin, A., Li, L., Peyton, M., Minna, J. D., Harran, P. G., & Wang, X. (2007) · Cancer Cell · doi:10.1016/j.ccr.2007.08.029 · Cited by 572 · see citing works

The inhibitors of apoptosis (IAPs) as cancer targets

Hunter, A. M., LaCasse, E. C., & Korneluk, R. G. (2007) · Apoptosis · doi:10.1007/s10495-007-0087-3 · Cited by 565 · see citing works

XIAP inhibits caspase‐3 and ‐7 using two binding sites: evolutionarily conserved mechanism of IAPs

Scott, F. L., Denault, J., Riedl, S. J., Shin, H., Renatus, M., & Salvesen, G. S. (2005) · The EMBO Journal · doi:10.1038/sj.emboj.7600544 · Cited by 420 · see citing works

Discovery of Potent Antagonists of the Antiapoptotic Protein XIAP for the Treatment of Cancer

Oost, T. K., Sun, C. C., Armstrong, R. C., Al-Assaad, A.-S., Betz, S. F., Deckwerth, T. L., Ding, H., Elmore, S. W., Meadows, R. P., Olejniczak, E. T., et al. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm040037k · Cited by 367 · see citing works

A novel one-step, highly sensitive fluorometric assay to evaluate cell-mediated cytotoxicity

Nociari, M., Shalev, A., Benias, P. C., & Russo, C. (1998) · Journal of Immunological Methods · doi:10.1016/s0022-1759(98)00028-3 · Cited by 351 · see citing works

Inhomogeneous Fluid Approach to Solvation Thermodynamics. 1. Theory

Lazaridis, T. (1998) · The Journal of Physical Chemistry B · doi:10.1021/jp9723574 · Cited by 334 · see citing works

A Potent and Orally Active Antagonist (SM-406/AT-406) of Multiple Inhibitor of Apoptosis Proteins (IAPs) in Clinical Development for Cancer Treatment

Cai, Q., Sun, H., Peng, Y., Lü, J., Nikolovska‐Coleska, Z., McEachern, D., Liu, L., Qiu, S., Yang, C., Miller, R. S., et al. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm101505d · Cited by 274 · see citing works

Translational upregulation of X-linked inhibitor of apoptosis (XIAP) increases resistance to radiation induced cell death

Holčı́k, M., Yeh, C., Korneluk, R. G., & Chow, T. Y.-K. (2000) · Oncogene · doi:10.1038/sj.onc.1203765 · Cited by 258 · see citing works

X-Linked Inhibitor of Apoptosis Protein – A Critical Death Resistance Regulator and Therapeutic Target for Personalized Cancer Therapy

Obexer, P., & Ausserlechner, M. J. (2014) · Frontiers in Oncology · doi:10.3389/fonc.2014.00197 · Cited by 245 · see citing works

Pd‐PEPPSI Complexes and the Negishi Reaction

Valente, C., Belowich, M. E., Hadei, N., et al. (2010) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201000359 · Cited by 222 · see citing works

Small-molecule SMAC mimetics as new cancer therapeutics

Bai, L., Smith, D. C., & Wang, S. (2014) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2014.05.007 · Cited by 211 · see citing works

Smac Mimetics Activate the E3 Ligase Activity of cIAP1 Protein by Promoting RING Domain Dimerization

Feltham, R., Bettjeman, B., Budhidarmo, R., Mace, P. D., Shirley, S., Condon, S. M., Chunduru, S. K., McKinlay, M. A., Vaux, D. L., Silke, J., et al. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.222919 · Cited by 168 · see citing works

Birinapant, a Smac-Mimetic with Improved Tolerability for the Treatment of Solid Tumors and Hematological Malignancies

Condon, S. M., Mitsuuchi, Y., Deng, Y., LaPorte, M. G., Rippin, S. R., Haimowitz, T., Alexander, M. D., Kumar, P. T., Hendi, M. S., Lee, Y.-H., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500176w · Cited by 153 · see citing works

IAP proteins as targets for drug development in oncology

Dubrez, L., Berthelet, J., & Glorian, V. (2013) · OncoTargets and Therapy · doi:10.2147/ott.s33375 · Cited by 133 · see citing works

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

Chessari, G., Buck, I. M., Day, J. E. H., Day, P. J., Iqbal, A., Johnson, C. N., Lewis, E. J., Martins, V., Miller, D., Reader, M., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00706 · Cited by 90 · see citing works

Learning and Confirming with Preclinical Studies: Modeling and Simulation in the Discovery of GDC-0917, an Inhibitor of Apoptosis Proteins Antagonist

Wong, H., Gould, S. E., Budha, N. R., Darbonne, W. C., Kadel, E. E., La, H., Alicke, B., Halladay, J. S., Erickson, R., Portera, C. C., et al. (2013) · Drug Metabolism and Disposition · doi:10.1124/dmd.113.053926 · Cited by 54 · see citing works

SAHA overcomes FLIP-mediated inhibition of SMAC mimetic-induced apoptosis in mesothelioma

Crawford, N., Stasik, I., Holohan, C., Majkut, J., McGrath, M., Johnston, P. G., Chessari, G., Ward, G. A., Waugh, D. J. J., Fennell, D. A., et al. (2013) · Cell Death and Disease · doi:10.1038/cddis.2013.258 · Cited by 40 · see citing works

Design and Synthesis of Potent Inhibitor of Apoptosis (IAP) Proteins Antagonists Bearing an Octahydropyrrolo[1,2-a]pyrazine Scaffold as a Novel Proline Mimetic

Hashimoto, K., Saito, B., Miyamoto, N., Oguro, Y., Tomita, D., Shiokawa, Z., Asano, M., Kakei, H., Taya, N., Kawasaki, M., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm301674z · Cited by 33 · see citing works

Inhibitor design by wrapping packing defects in HIV-1 proteins

Fernández, A., Rogale, K., Scott, R., & Scheraga, H. A. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0404641101 · Cited by 31 · see citing works

A web-based platform for virtual screening

Watson, P., Verdonk, M. L., & Hartshorn, M. J. (2003) · Journal of Molecular Graphics and Modelling · doi:10.1016/s1093-3263(03)00137-2 · Cited by 27 · see citing works

Time‐Dependent Inhibition and Induction of Human Cytochrome P4503A4/5 by an Oral IAP Antagonist, LCL161, In Vitro and In Vivo in Healthy Subjects

Dhuria, S. V., Einolf, H. J., Mangold, J. B., Sen, S., Gu, H., Wang, L., & Cameron, S. B. (2013) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.79 · Cited by 23 · see citing works

The Synthesis of 3,3-Dimethyl Aza- and Diazaindolines Using a Palladium-Catalysed Intramolecular Reductive Cyclisation

Day, J. E. H., Frederickson, M., Hogg, C., et al. (2015) · Synlett · doi:10.1055/s-0035-1560320 · Cited by 10 · see citing works

Targeted protein degradation: expanding the toolbox

Schapira, M., Calabrese, M. F., Bullock, A. N., & Crews, C. M. (2019) · Nature Reviews Drug Discovery · doi:10.1038/s41573-019-0047-y · Cited by 960 · see citing works

Protein posttranslational modifications in health and diseases: Functions, regulatory mechanisms, and therapeutic implications

Zhong, Q., Xiao, X., Qiu, Y., Xu, Z., Chen, C., Chong, B., Zhao, X., Hai, S., Li, S., An, Z., et al. (2023) · MedComm · doi:10.1002/mco2.261 · Cited by 442 · see citing works

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

Schiemer, J., Horst, R., Meng, Y., Montgomery, J. I., Xu, Y., Feng, X., Borzilleri, K., Uccello, D. P., Leverett, C., Brown, S., et al. (2021) · Nature Chemical Biology · doi:10.1038/s41589-020-00686-2 · Cited by 113 · see citing works

Small molecules targeting protein–protein interactions for cancer therapy

Wu, D., Li, Y., Zheng, L., Xiao, H., Ouyang, L., Wang, G., & Sun, Q. (2023) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2023.05.035 · Cited by 71 · see citing works

Therapeutics Targeting the Core Apoptotic Machinery

Hamilton, C., Fox, J. P., Longley, D. B., & Higgins, C. A. (2021) · Cancers · doi:10.3390/cancers13112618 · Cited by 26 · see citing works

Faculty Opinions recommendation of Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).

Congreve, M., & Pickworth, M. (2017) · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature · doi:10.3410/f.727604992.793532954

Influence of caspase-binding ability of the X-linked Inhibitor of Apoptosis Protein (XIAP) on serine protease inhibitor-sensitive apoptosis

Walliser, M. (2005)

The Serine Protease Omi/HtrA2 Regulates Apoptosis by Binding XIAP through a Reaper-like Motif

Martins, L. M., Iaccarino, I., Tenev, T., Gschmeissner, S., Totty, N. F., Lemoine, N. R., Savopoulos, J. W., Gray, C. W., Creasy, C. L., Dingwall, C., et al. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m109784200 · Cited by 544 · see citing works

Apoptotic sensitivity of murine IAP-deficient cells

Rumble, J. M., Bertrand, M. J. M., Csomos, R. A., Wright, C. W., Albert, L., Mak, T. W., Barker, P. A., & Duckett, C. S. (2008) · Biochemical Journal · doi:10.1042/bj20081188 · Cited by 19 · see citing works

X-linked Inhibitor of Apoptosis Protein (XIAP) Inhibits Caspase-3 and -7 in Distinct Modes

Suzuki, Y., Nakabayashi, Y., Nakata, K., Reed, J. C., & Takahashi, R. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m102415200 · Cited by 235 · see citing works