Page last updated: 2024-08-21

thiazoles and lcl161

thiazoles has been researched along with lcl161 in 56 studies

Research

Studies (56)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's38 (67.86)24.3611
2020's18 (32.14)2.80

Authors

AuthorsStudies
Chen, KF; Chen, PJ; Cheng, AL; Lin, JP; Liu, CY; Shiau, CW; Tai, WT; Yu, HC1
Cebon, J; Fucikova, J; Knights, AJ; Koernig, S; Pasam, A1
Adem, A; Alemu, G; Arap, W; Barrett, CJ; Cho, H; Geha, R; Libutti, SK; Pasqualini, R; Pastoriza, J; Quinn, TJ; Smith, T; Syrkin, G; Vrikshajanani, C; Yuan, Z1
Cameron, S; Dhuria, S; Einolf, H; Gu, H; Mangold, J; Sen, S; Wang, L1
Engert, A; Gasser, S; Hansen, HP; Reiners, KS; Sauer, M; von Strandmann, EP1
Cai, J; Dai, S; Liu, J; Liu, Z; Lu, J; Ma, J; Qin, Q; Sun, X; Tao, G; Xu, L; Yang, X; Zhan, L; Zhang, C; Zhang, X; Zhu, H; Zuo, Y1
Haug, J; Kimlinger, T; Kumar, S; Painuly, U; Rajkumar, SV; Ramakrishnan, V1
Beug, ST; Cowan, KN; Earl, N; Faye, MD; Graber, TE; Holcik, M; Korneluk, RG; Langlois, S; Michaud, J; Wild, B; Xiang, X1
Duan, W; George, J; Hebbard, L; Hu, Z; Lie, S; Qiao, L; Tian, A; Wilson, GS; Wu, G1
Cameron, S; Cohen, RB; Dees, EC; Dhuria, SV; Infante, JR; Olszanski, AJ; Sen, S1
Fulda, S1
Cutts, SM; Green, MM; Hawkins, CJ; Miles, MA; Rayner, DM; Shekhar, TM1
Han, F; Hu, J; Jin, G; Lan, Y; Liu, H; Liu, X; Liu, Z; Sun, Y; Wang, B; Zhang, M; Zhang, X1
Belz, K; Fulda, S; Haß, C; Schoeneberger, H1
Brands, RC; Hartmann, S; Herbst, F; Kübler, AC; Linz, C; Müller-Richter, UDA; Seher, A1
Gupte, A; Hawkins, CJ; Miles, MA; Shekhar, TM; Tascone, B; Taylor, S; Walkley, CR1
Bi, L; Gomez, M; Haug, J; Kimlinger, T; Kumar, S; Mukhopadhyay, B; Painuly, U; Prasad, V; Rajkumar, SV; Ramakrishnan, V1
Chen, SM; Hsieh, LL; Huang, SF; Li, YY; Lui, TN; Salazar, N; Tseng, YY; Tu, CH1
Chong, D; Liu, H; Ma, L; Ren, K; Zhang, Z; Zhao, S; Zhou, C1
Appl, B; Eschenburg, G; Hundsdoerfer, P; Langemann, D; Najem, S; Reinshagen, K; Trochimiuk, M1
Chen, Y; Nan, K; Qin, S; Ren, H; Sun, X; Wang, H; Xiao, G; Yang, C; Zhang, B; Zhang, Y1
Ahmann, GJ; Ailawadhi, S; Akhmetzyanova, I; Asmann, YW; Bergsagel, PL; Buadi, F; Calcinotto, A; Chanan-Khan, AA; Chesi, M; Dingli, D; Dispenzieri, A; Dueck, AC; Fonseca, R; Fooksman, D; Garbitt, VM; Gertz, MA; Keane, N; Kosiorek, HE; Kumar, SK; Lacy, MQ; Lin, Y; Mirza, NN; Morrison, KM; Reeder, CB; Riggs, DL; Sharik, ME; Stewart, AK1
Bode, KJ; Brunner, T; Delgado, ME; Demgenski, J; Etemadi, N; Grabinger, T; Hänggi, K; Hauck, C; Knop, J; Kostadinova, F; Nachbur, U; Reinhold, C; Schweinlin, M; Seitz, C; Silke, J; W Wei-Lynn, W; Wajant, H; Walles, H; Wilhelm, S1
Miura, K; Philchenkov, A1
Beug, ST; Chabot, J; Dobson, CC; Faye, MD; Holcik, M; Korneluk, RG; LaCasse, EC; Naing, T; St-Jean, M; Stojdl, DF; Walker, DE1
Alain, T; Beauregard, CE; Beug, ST; Chabot, J; Earl, N; Forsyth, PA; Healy, C; Korneluk, RG; LaCasse, EC; Lun, X; Mohan, A; Robbins, SM; Sanda, T; Senger, DL; St-Jean, M; Staeheli, P; Walker, DE1
Cyr, DM; Grove, DE; Ren, HY; Sopha, P1
Cho, N; Hattori, T; Imaeda, Y; Miyamoto, N; Nagai, K; Naito, M; Nara, H; Ohoka, N; Sameshima, T; Shibata, N; Shimokawa, K1
Balce, DR; Dastidar, H; Ernst, M; Ewanchuk, BW; Gafuik, C; Jenne, C; Kim, DS; Lau, K; Mahoney, DJ; Naumenko, V; Rajwani, J; Rakic, A; Sikdar, S; Tailor, P; Yates, RM; Zemp, FJ; Zhang, C1
Athineos, D; Binks, A; Blyth, K; Dowson, S; Ennis, D; Leung, EYL; McNeish, IA; Mullin, M; Orange, C; Tait, SWG; Walton, JB; Weigert, M; Yu, X1
Appl, B; Eschenburg, G; Frommann, K; Hundsdoerfer, P; Reinshagen, K1
Cho, N; Fujimori, I; Hattori, T; Hayase, Y; Imaeda, Y; Ito, M; Koyama, R; Morita, Y; Nagai, K; Naito, M; Nara, H; Ohoka, N; Okuhira, K; Sameshima, T; Sano, O; Shibata, N; Shimokawa, K; Ujikawa, O1
Czaplinski, S; Fulda, S; Habermann, K; Hugle, M; Vogler, M1
Barth, MJ; Gu, JJ; Hernandez-Ilizaliturri, FJ; Mavis, C; Runckel, K1
Fukano, M; Holbrook, J; Korneluk, RG; LaCasse, EC; Lala-Tabbert, N; Lejmi-Mrad, R; St-Jean, M; Timusk, K1
Jin, G; Liu, Y; Xu, P1
Guo, H; Hartkamp, J; Krämer, OH; Lüscher, B; Treude, F1
Burvenich, IJG; Harris, MA; Hawkins, CJ; Parker, BS; Rigopoulos, A; Scott, AM; Shekhar, TM; Spurling, A; Walkley, CR; Zanker, D1
Boldrin, E; Debatin, KM; Fischer-Posovszky, P; Kestler, HA; Kraus, JM; Meyer, LH; Meyer, M; Schlichtig, F; Zinngrebe, J1
Koch, PD; Kohler, RH; Pittet, MJ; Rodell, CB; Weissleder, R1
Berg, M; Cinatl, J; Michaelis, M; Rothweiler, F; Stege, H; Vallo, S; Winkelmann, R1
Jin, G; Liu, X; Liu, Y; Wang, K; Zhang, H; Zhang, X1
Allison, C; Arandjelovic, P; Boddey, JA; Doerflinger, M; Ebert, G; Erickson, S; Ioannidis, L; Lopaticki, S; Mackiewicz, L; O'Neill, MT; Pellegrini, M; Rajasekaran, P; Silke, J; Steel, RWJ; Yang, ASP1
Chang, JY; Chang, YC; Cheng, SM; Cheung, CHA; Coumar, MS; Kondapuram, SK; Leung, E; Lin, TY; Lin, YC; Syed, SB; Yang, TH1
Hawkins, CJ; Miles, MA1
Choi, J; Han, D; Hwang, EH; Im, SA; Kang, SE; Kim, K; Lee, H; Lee, KH; Lee, KM; Moon, WK; Oh, HJ; Ryu, HS1
Granqvist, V; Holmgren, C; Larsson, C1
Ahn, SH; Clark, MP; Earnest, L; Ebert, G; Huynh, T; Littlejohn, M; Mackiewicz, L; Mahmoudi, T; Mason, H; Netter, HJ; Pellegrini, M; Rao, S; Revill, P; Romal, S; Sozzi, V; Stutz, MD; Torresi, J; Tran, BM; Vincan, E; Wiedemann, N1
Allison, CC; Arandjelovic, P; Asselin-Labat, ML; Bader, SM; Batey, D; Doerflinger, M; Herold, MJ; Ojaimi, S; Pellegrini, M; Preston, SP; Strasser, A; Stutz, MD; West, NP; Whitehead, L1
Cerra, C; Harris, MA; Hawkins, CJ; Miles, MA; Shekhar, TM1
Bledsoe, S; Borthakur, GM; Bose, P; Bueso-Ramos, CE; Carter, BZ; Cortes, J; Daver, NG; DiNardo, CD; Estrov, ZE; Garcia-Manero, G; Jabbour, E; Jain, N; Kadia, TM; Konopleva, MY; Mak, PY; Masarova, L; Ohanian, M; Pemmaraju, N; Pierce, S; Popat, U; Qiao, W; Verstovsek, S; Wang, X; Zhou, L1
Demizu, Y; Fukuhara, K; Inoue, T; Ito, T; Kurohara, T; Naito, M; Ohoka, N; Takyo, M; Tsuchiya, K; Yokoo, H1
Abildgaard, A; Bergsland, CH; Eide, PW; Guren, MG; Kryeziu, K; Lassen, K; Lothe, RA; Moosavi, SH; Nesbakken, A; Sveen, A; Totland, MZ1
Cao, H; Cheng, Q; Dai, Z; Liu, Y; Liu, Z; Mo, Y; Wang, Z; Ye, W; Zhang, H; Zhang, X1
Ando, Y; Kiyota, N; Minami, H; Mitsuma, A; Morita, S; Toyoda, M1
Campbell, GR; Cartier, J; Causse, SZ; Dubrez, L; Gaurav, N; Hawkins, CJ; Holt, TA; Klein, BJ; Kutateladze, TG; Miles, MA; Shi, X; Spector, SA; Tencer, AH; Wen, H; Xuan, H; Yu, Y; Zadoroznyj, A1

Reviews

1 review(s) available for thiazoles and lcl161

ArticleYear
The IAP Protein Family, SMAC Mimetics and Cancer Treatment.
    Critical reviews in oncogenesis, 2016, Volume: 21, Issue:3-4

    Topics: Antineoplastic Agents; Apoptosis; Azocines; Benzhydryl Compounds; Cell Proliferation; Dipeptides; Humans; Indoles; Inhibitor of Apoptosis Proteins; Neoplasms; Thiazoles

2016

Trials

4 trial(s) available for thiazoles and lcl161

ArticleYear
Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2014, Oct-01, Volume: 32, Issue:28

    Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Antineoplastic Agents; Area Under Curve; Biological Availability; Cytokines; Diarrhea; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Humans; Inhibitor of Apoptosis Proteins; Male; Middle Aged; Nausea; Neoplasms; Pharmaceutical Solutions; Syndrome; Tablets; Thiazoles; Treatment Outcome; Vomiting

2014
IAP antagonists induce anti-tumor immunity in multiple myeloma.
    Nature medicine, 2016, Volume: 22, Issue:12

    Topics: Aged; Aged, 80 and over; Animals; Antineoplastic Agents; Cell Line, Tumor; Cyclophosphamide; Dendritic Cells; Disease Models, Animal; Female; Gene Expression; Humans; Inhibitor of Apoptosis Proteins; Interferon Type I; Macrophages; Male; Mice; Mice, Transgenic; Middle Aged; Multiple Myeloma; Neoplasm Recurrence, Local; Phagocytosis; Thiazoles

2016
Final results of a phase 2 clinical trial of LCL161, an oral SMAC mimetic for patients with myelofibrosis.
    Blood advances, 2021, 08-24, Volume: 5, Issue:16

    Topics: Apoptosis; Humans; Myeloproliferative Disorders; Primary Myelofibrosis; Thiazoles

2021
A phase I study of LCL161, a novel oral pan-inhibitor of apoptosis protein (IAP) antagonist, in Japanese patients with advanced solid tumors.
    Asia-Pacific journal of clinical oncology, 2022, Volume: 18, Issue:5

    Topics: Bayes Theorem; Humans; Inhibitor of Apoptosis Proteins; Japan; Neoplasms; Paclitaxel; Thiazoles; Treatment Outcome

2022

Other Studies

51 other study(ies) available for thiazoles and lcl161

ArticleYear
Inhibition of Bcl-2 improves effect of LCL161, a SMAC mimetic, in hepatocellular carcinoma cells.
    Biochemical pharmacology, 2012, Aug-01, Volume: 84, Issue:3

    Topics: Animals; Antineoplastic Agents; Biomimetic Materials; Carcinoma, Hepatocellular; Down-Regulation; HEK293 Cells; Humans; Liver Neoplasms, Experimental; Male; Mice; Mice, Nude; Oligopeptides; Proto-Oncogene Proteins c-bcl-2; Pyrroles; Thiazoles; Treatment Outcome; Xenograft Model Antitumor Assays

2012
Inhibitor of apoptosis protein (IAP) antagonists demonstrate divergent immunomodulatory properties in human immune subsets with implications for combination therapy.
    Cancer immunology, immunotherapy : CII, 2013, Volume: 62, Issue:2

    Topics: Antigens, Neoplasm; Antineoplastic Agents; Apoptosis; Cancer Vaccines; Cells, Cultured; Combined Modality Therapy; Cytokines; Dendritic Cells; Humans; Immunotherapy; Inhibitor of Apoptosis Proteins; Leukocytes, Mononuclear; NF-kappa B; Peptides; T-Lymphocytes; Thiazoles; Up-Regulation

2013
Blockade of inhibitors of apoptosis (IAPs) in combination with tumor-targeted delivery of tumor necrosis factor-α leads to synergistic antitumor activity.
    Cancer gene therapy, 2013, Volume: 20, Issue:1

    Topics: Administration, Oral; Animals; Antineoplastic Agents; Apoptosis; Caspases; Cell Line, Tumor; Cell Proliferation; Combined Modality Therapy; Dependovirus; Drug Resistance, Neoplasm; Female; Genetic Therapy; Humans; Inhibitor of Apoptosis Proteins; Melanoma; Mice; Mice, Nude; Organ Specificity; Proteolysis; Thiazoles; Transduction, Genetic; Tumor Burden; Tumor Necrosis Factor-alpha; Xenograft Model Antitumor Assays

2013
Time-dependent inhibition and induction of human cytochrome P4503A4/5 by an oral IAP antagonist, LCL161, in vitro and in vivo in healthy subjects.
    Journal of clinical pharmacology, 2013, Volume: 53, Issue:6

    Topics: Adult; Area Under Curve; Cytochrome P-450 CYP3A; Dose-Response Relationship, Drug; Drug Interactions; Enzyme Induction; Enzyme Inhibitors; Female; Hepatocytes; Humans; Inhibitor of Apoptosis Proteins; Male; Microsomes, Liver; Midazolam; Middle Aged; Models, Biological; Pregnane X Receptor; Receptors, Steroid; RNA, Messenger; Thiazoles; Time Factors; Young Adult

2013
Induction of the DNA damage response by IAP inhibition triggers natural immunity via upregulation of NKG2D ligands in Hodgkin lymphoma in vitro.
    Biological chemistry, 2013, Volume: 394, Issue:10

    Topics: Blotting, Western; Cell Line, Tumor; DNA Damage; Enzyme-Linked Immunosorbent Assay; Flow Cytometry; Gene Expression Regulation, Neoplastic; Hodgkin Disease; Humans; Immunity, Innate; Inhibitor of Apoptosis Proteins; NK Cell Lectin-Like Receptor Subfamily K; Thiazoles; Tumor Necrosis Factor-alpha; Up-Regulation

2013
Smac mimetic compound LCL161 sensitizes esophageal carcinoma cells to radiotherapy by inhibiting the expression of inhibitor of apoptosis protein.
    Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine, 2014, Volume: 35, Issue:3

    Topics: Apoptosis; Apoptosis Regulatory Proteins; Biomimetics; Blotting, Western; Carcinoma, Squamous Cell; Cell Line, Tumor; Enzyme-Linked Immunosorbent Assay; Esophageal Neoplasms; Esophageal Squamous Cell Carcinoma; Flow Cytometry; Fluorescent Antibody Technique; Humans; Inhibitor of Apoptosis Proteins; Intracellular Signaling Peptides and Proteins; Mitochondrial Proteins; Radiation-Sensitizing Agents; Reverse Transcriptase Polymerase Chain Reaction; Thiazoles; Ubiquitin-Protein Ligases

2014
Inhibitor of apoptosis proteins as therapeutic targets in multiple myeloma.
    Leukemia, 2014, Volume: 28, Issue:7

    Topics: Antineoplastic Agents; Apoptosis; Apoptosis Regulatory Proteins; Caspases; Cell Death; Cell Line, Tumor; Cell Proliferation; Enzyme Activation; Fas Ligand Protein; Humans; Janus Kinase 2; Molecular Targeted Therapy; Multiple Myeloma; NF-kappa B; Signal Transduction; STAT3 Transcription Factor; Thiazoles; TNF-Related Apoptosis-Inducing Ligand; Tumor Microenvironment

2014
IGF2BP1 controls cell death and drug resistance in rhabdomyosarcomas by regulating translation of cIAP1.
    Oncogene, 2015, Mar-19, Volume: 34, Issue:12

    Topics: Alkynes; Animals; Apoptosis; Cell Line, Tumor; Dipeptides; Drug Resistance, Neoplasm; Female; Gene Expression Regulation, Neoplastic; HEK293 Cells; Humans; Inhibitor of Apoptosis Proteins; Mice; Mice, Nude; Neoplasm Transplantation; Protein Biosynthesis; Rhabdomyosarcoma; RNA-Binding Proteins; Signal Transduction; Thiazoles; Tumor Necrosis Factor-alpha; Ubiquitin-Protein Ligases

2015
Synergistic effects of IAP inhibitor LCL161 and paclitaxel on hepatocellular carcinoma cells.
    Cancer letters, 2014, Sep-01, Volume: 351, Issue:2

    Topics: Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Hepatocellular; Cell Growth Processes; Cell Line, Tumor; Drug Synergism; Humans; Inhibitor of Apoptosis Proteins; Liver Neoplasms; Paclitaxel; Proto-Oncogene Proteins c-bcl-2; Thiazoles

2014
Targeting inhibitor of apoptosis proteins for cancer therapy: a double-edge sword?
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2014, Oct-01, Volume: 32, Issue:28

    Topics: Antineoplastic Agents; Female; Humans; Inhibitor of Apoptosis Proteins; Male; Neoplasms; Thiazoles

2014
Inhibition of Bcl-2 or IAP proteins does not provoke mutations in surviving cells.
    Mutation research, 2015, Volume: 777

    Topics: Animals; Antineoplastic Agents; Apoptosis; Azocines; bcl-2-Associated X Protein; Benzhydryl Compounds; Biphenyl Compounds; Cell Line, Tumor; Cell Survival; Comet Assay; DNA Damage; Dose-Response Relationship, Drug; Inhibitor of Apoptosis Proteins; Mice; Mutagens; Mutation; Nitrophenols; Piperazines; Sulfonamides; Thiazoles

2015
Smac mimetic‑induced caspase‑independent necroptosis requires RIP1 in breast cancer.
    Molecular medicine reports, 2016, Volume: 13, Issue:1

    Topics: Amino Acid Chloromethyl Ketones; Apoptosis; Breast Neoplasms; Caspase Inhibitors; Caspases; Cell Proliferation; Female; Humans; Inhibitor of Apoptosis Proteins; MCF-7 Cells; Membrane Potential, Mitochondrial; Necrosis; Nuclear Pore Complex Proteins; Proteolysis; RNA-Binding Proteins; Thiazoles

2016
Sensitization of acute lymphoblastic leukemia cells for LCL161-induced cell death by targeting redox homeostasis.
    Biochemical pharmacology, 2016, Apr-01, Volume: 105

    Topics: Antineoplastic Agents; Apoptosis; Cell Death; Cell Survival; Dose-Response Relationship, Drug; Drug Delivery Systems; Homeostasis; Humans; Jurkat Cells; Methionine; Oxidation-Reduction; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Reactive Oxygen Species; Sulfoxides; Thiazoles

2016
Cytotoxic effects of SMAC-mimetic compound LCL161 in head and neck cancer cell lines.
    Clinical oral investigations, 2016, Volume: 20, Issue:9

    Topics: Apoptosis; Blotting, Western; Carcinoma, Squamous Cell; Cell Line, Tumor; Drug Therapy, Combination; Fas Ligand Protein; fas Receptor; Flow Cytometry; Head and Neck Neoplasms; Humans; Inhibitor of Apoptosis Proteins; Thiazoles

2016
IAP antagonists sensitize murine osteosarcoma cells to killing by TNFα.
    Oncotarget, 2016, Jun-07, Volume: 7, Issue:23

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Baculoviral IAP Repeat-Containing 3 Protein; Bone Neoplasms; Bridged Bicyclo Compounds, Heterocyclic; Cell Line, Tumor; Cell Survival; Cyclohexanes; Dose-Response Relationship, Drug; Genetic Predisposition to Disease; HEK293 Cells; Humans; Inhibitor of Apoptosis Proteins; Mice, Knockout; Osteosarcoma; Phenotype; Pyrroles; Receptor-Interacting Protein Serine-Threonine Kinases; Retinoblastoma Protein; Signal Transduction; Thiazoles; TNF-Related Apoptosis-Inducing Ligand; Transfection; Triazoles; Tumor Necrosis Factor-alpha; Tumor Suppressor Protein p53; Ubiquitin-Protein Ligases

2016
Smac mimetic LCL161 overcomes protective ER stress induced by obatoclax, synergistically causing cell death in multiple myeloma.
    Oncotarget, 2016, Aug-30, Volume: 7, Issue:35

    Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Apoptosis Regulatory Proteins; Caspases; Cell Line, Tumor; Down-Regulation; Drug Resistance, Neoplasm; Drug Synergism; Endoplasmic Reticulum Chaperone BiP; Endoplasmic Reticulum Stress; Heat-Shock Proteins; Humans; Indoles; Intracellular Signaling Peptides and Proteins; Mitochondrial Proteins; Multiple Myeloma; Neoplasm Recurrence, Local; Phosphatidylinositol 3-Kinases; Phosphorylation; Proto-Oncogene Proteins c-akt; Proto-Oncogene Proteins c-bcl-2; Pyrroles; Thiazoles; Unfolded Protein Response; Up-Regulation; X-Box Binding Protein 1

2016
Blockade of Inhibitors of Apoptosis Proteins in Combination with Conventional Chemotherapy Leads to Synergistic Antitumor Activity in Medulloblastoma and Cancer Stem-Like Cells.
    PloS one, 2016, Volume: 11, Issue:8

    Topics: Antineoplastic Agents; Apoptosis; Autophagy; Caspase 3; Caspase 7; Cell Line, Tumor; Cell Survival; Cerebellar Neoplasms; Cisplatin; Drug Synergism; Drug Therapy, Combination; Humans; Medulloblastoma; Neoplastic Stem Cells; Oligopeptides; Thiazoles; Vincristine

2016
[Effects of LCL161, a Smac mimetic on the proliferation and apoptosis in hepatocellular carcinoma cells].
    Zhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences, 2016, Sep-28, Volume: 41, Issue:9

    Topics: Apoptosis; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Proliferation; Cell Survival; Down-Regulation; Hep G2 Cells; Humans; Inhibitor of Apoptosis Proteins; Liver Neoplasms; Membrane Potential, Mitochondrial; Proto-Oncogene Proteins c-akt; Thiazoles; Ubiquitin-Protein Ligases; X-Linked Inhibitor of Apoptosis Protein

2016
Smac mimetic LCL161 supports neuroblastoma chemotherapy in a drug class-dependent manner and synergistically interacts with ALK inhibitor TAE684 in cells with ALK mutation F1174L.
    Oncotarget, 2016, Nov-08, Volume: 7, Issue:45

    Topics: Anaplastic Lymphoma Kinase; Cell Line, Tumor; Humans; Mutation; Neuroblastoma; Protein Kinase Inhibitors; Pyrimidines; Receptor Protein-Tyrosine Kinases; Thiazoles

2016
LCL161 increases paclitaxel-induced apoptosis by degrading cIAP1 and cIAP2 in NSCLC.
    Journal of experimental & clinical cancer research : CR, 2016, 09-30, Volume: 35, Issue:1

    Topics: Adult; Aged; Animals; Antineoplastic Combined Chemotherapy Protocols; Baculoviral IAP Repeat-Containing 3 Protein; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Cell Survival; Drug Synergism; Female; Gene Expression Regulation, Neoplastic; Humans; Inhibitor of Apoptosis Proteins; Lung Neoplasms; Male; Mice; Middle Aged; Paclitaxel; Prognosis; Proteolysis; Thiazoles; Treatment Outcome; Ubiquitin-Protein Ligases; Up-Regulation; Xenograft Model Antitumor Assays

2016
Inhibitor of Apoptosis Protein-1 Regulates Tumor Necrosis Factor-Mediated Destruction of Intestinal Epithelial Cells.
    Gastroenterology, 2017, Volume: 152, Issue:4

    Topics: Animals; Apoptosis; Baculoviral IAP Repeat-Containing 3 Protein; Cell Death; Cell Line, Tumor; Cytokine TWEAK; Epithelial Cells; Humans; Inhibitor of Apoptosis Proteins; Intestinal Mucosa; Liver; Macrophages; Mice; Mice, Inbred C57BL; Mice, Knockout; Organoids; Receptors, Tumor Necrosis Factor, Type I; Receptors, Tumor Necrosis Factor, Type II; Thiazoles; Tumor Necrosis Factor-alpha; Tumor Necrosis Factors; Ubiquitin-Protein Ligases

2017
Oncolytic virus synergizes with Smac mimetic compounds to induce rhabdomyosarcoma cell death in a syngeneic murine model.
    Oncotarget, 2017, Jan-10, Volume: 8, Issue:2

    Topics: Animals; Cell Death; Cell Line, Tumor; Cell Survival; Combined Modality Therapy; Disease Models, Animal; Female; Humans; Immunity, Innate; Interferon Regulatory Factor-1; Mice; Molecular Mimicry; Oncolytic Virotherapy; Oncolytic Viruses; Rhabdomyosarcoma; Thiazoles; Tumor Burden; Tumor Necrosis Factor-alpha; Xenograft Model Antitumor Assays

2017
Smac mimetics synergize with immune checkpoint inhibitors to promote tumour immunity against glioblastoma.
    Nature communications, 2017, 02-15, Volume: 8

    Topics: Adaptive Immunity; Animals; Antineoplastic Agents; B7-H1 Antigen; Brain Neoplasms; Cell Line, Tumor; Female; Gene Expression Regulation; Genetic Vectors; Glioblastoma; Humans; Immunity, Innate; Immunologic Memory; Inhibitor of Apoptosis Proteins; Interferon-alpha; Interferon-beta; Mice; Poly I-C; Signal Transduction; Survival Analysis; T-Lymphocytes, Cytotoxic; Thiazoles; Tumor Necrosis Factor-alpha; Vesiculovirus; Xenograft Model Antitumor Assays

2017
Endoplasmic reticulum stress-induced degradation of DNAJB12 stimulates BOK accumulation and primes cancer cells for apoptosis.
    The Journal of biological chemistry, 2017, 07-14, Volume: 292, Issue:28

    Topics: Amino Acid Substitution; Animals; Antineoplastic Agents; Apoptosis; Carcinoma, Hepatocellular; Cell Line, Tumor; Chlorocebus aethiops; COS Cells; Drug Resistance, Neoplasm; Endoplasmic Reticulum Stress; HEK293 Cells; HSP40 Heat-Shock Proteins; Humans; Liver Neoplasms; Mutation; Neoplasm Proteins; Proteasome Endopeptidase Complex; Protein Stability; Proteolysis; Proto-Oncogene Proteins c-bcl-2; Receptors, Autocrine Motility Factor; Recombinant Fusion Proteins; RNA Interference; Thiazoles

2017
Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands.
    Cancer science, 2017, Volume: 108, Issue:8

    Topics: Cell Line, Tumor; Cell Proliferation; Cell Survival; Dasatinib; Down-Regulation; Fusion Proteins, bcr-abl; Gene Expression Regulation, Neoplastic; Humans; Inhibitor of Apoptosis Proteins; K562 Cells; Ligands; Phosphorylation; Protein Binding; Protein Kinase Inhibitors; Proteolysis; Proto-Oncogene Mas; Thiazoles; Ubiquitination

2017
Smac mimetics and oncolytic viruses synergize in driving anticancer T-cell responses through complementary mechanisms.
    Nature communications, 2017, 08-24, Volume: 8, Issue:1

    Topics: Animals; Antineoplastic Agents; Apoptosis Regulatory Proteins; Biomimetic Materials; CD8-Positive T-Lymphocytes; Cell Line, Tumor; Combined Modality Therapy; Female; Humans; Intracellular Signaling Peptides and Proteins; Mice; Mice, Inbred BALB C; Mice, Inbred C57BL; Mitochondrial Proteins; Neoplasms, Experimental; Oncolytic Virotherapy; Oncolytic Viruses; Thiazoles; Treatment Outcome; Vesicular stomatitis Indiana virus

2017
RIPK3 promotes adenovirus type 5 activity.
    Cell death & disease, 2017, 12-13, Volume: 8, Issue:12

    Topics: Adenoviruses, Human; Amino Acid Chloromethyl Ketones; Animals; Apoptosis; Base Sequence; Cell Line, Tumor; DNA, Viral; Female; Gene Expression Regulation; HEK293 Cells; HeLa Cells; Humans; Imidazoles; Indoles; Mice; Mice, Nude; Necrosis; Protein Kinases; Receptor-Interacting Protein Serine-Threonine Kinases; Sequence Deletion; Signal Transduction; Thiazoles; Tumor Necrosis Factor-alpha; Xenograft Model Antitumor Assays

2017
Vincristine resistance in relapsed neuroblastoma can be efficiently overcome by Smac mimetic LCL161 treatment.
    Journal of pediatric surgery, 2018, Volume: 53, Issue:10

    Topics: Apoptosis; Cell Line, Tumor; Cell Survival; Drug Resistance, Neoplasm; Humans; Neoplasm Recurrence, Local; Neuroblastoma; Thiazoles; Vincristine

2018
Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation.
    The Journal of biological chemistry, 2018, 05-04, Volume: 293, Issue:18

    Topics: Animals; Antineoplastic Agents; Down-Regulation; Estrogen Receptor alpha; Humans; Ligands; MCF-7 Cells; Mice; Protein Binding; Proteolysis; Thiazoles; Ubiquitination; X-Linked Inhibitor of Apoptosis Protein; Xenograft Model Antitumor Assays

2018
Identification of Smac mimetics as novel substrates for p-glycoprotein.
    Cancer letters, 2019, Volume: 440-441

    Topics: Apoptosis Regulatory Proteins; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biomimetic Materials; Cell Line, Tumor; Dipeptides; Doxorubicin; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Etoposide; Humans; Indoles; Inhibitor of Apoptosis Proteins; Intracellular Signaling Peptides and Proteins; Mitochondrial Proteins; Neuroblastoma; Oligopeptides; Rhabdomyosarcoma; Thiazoles; Up-Regulation; Vincristine

2019
The SMAC mimetic LCL-161 displays antitumor activity in preclinical models of rituximab-resistant B-cell lymphoma.
    Blood advances, 2018, 12-11, Volume: 2, Issue:23

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Disease Models, Animal; Drug Resistance, Neoplasm; Drug Therapy, Combination; Humans; Inhibitor of Apoptosis Proteins; Lymphoma, B-Cell; Mice; Mice, SCID; Oligopeptides; Proteasome Inhibitors; Proto-Oncogene Proteins c-bcl-2; Rituximab; Survivin; Thiazoles; Transplantation, Heterologous

2018
Targeted ablation of the cellular inhibitor of apoptosis 1 (cIAP1) attenuates denervation-induced skeletal muscle atrophy.
    Skeletal muscle, 2019, 05-24, Volume: 9, Issue:1

    Topics: Animals; Apoptosis Regulatory Proteins; Cell Line; Female; Gene Targeting; Humans; Inhibitor of Apoptosis Proteins; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Mitochondrial Proteins; Muscle Denervation; Muscular Atrophy; Myoblasts, Skeletal; NF-kappa B; Signal Transduction; Thiazoles; Up-Regulation

2019
Induction of Necroptosis in Human Breast Cancer Drug-Resistant Cells by SMAC Analog LCL161 After Caspase Inhibition Requires RIP3.
    Die Pharmazie, 2019, 06-01, Volume: 74, Issue:6

    Topics: Amino Acid Chloromethyl Ketones; Antineoplastic Agents; Apoptosis; Breast Neoplasms; Gene Knockdown Techniques; Humans; MCF-7 Cells; Mitochondria; Necroptosis; Receptor-Interacting Protein Serine-Threonine Kinases; RNA, Small Interfering; Thiazoles

2019
PAR-4 overcomes chemo-resistance in breast cancer cells by antagonizing cIAP1.
    Scientific reports, 2019, 06-19, Volume: 9, Issue:1

    Topics: Caspase 8; DNA Damage; Drug Resistance, Neoplasm; Female; Humans; Inhibitor of Apoptosis Proteins; MCF-7 Cells; Neoplasm Proteins; Receptors, Thrombin; Signal Transduction; Thiazoles; Triple Negative Breast Neoplasms; Ubiquitin-Protein Ligases

2019
Smac mimetics LCL161 and GDC-0152 inhibit osteosarcoma growth and metastasis in mice.
    BMC cancer, 2019, Sep-14, Volume: 19, Issue:1

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Cyclohexanes; Disease Models, Animal; Humans; Magnetic Resonance Imaging; Mice; Neoplasms; Positron-Emission Tomography; Pyrroles; Thiazoles; Xenograft Model Antitumor Assays

2019
Biomarker profile for prediction of response to SMAC mimetic monotherapy in pediatric precursor B-cell acute lymphoblastic leukemia.
    International journal of cancer, 2020, 06-01, Volume: 146, Issue:11

    Topics: Animals; Apoptosis; Apoptosis Regulatory Proteins; Azocines; Benzhydryl Compounds; Caspase Inhibitors; Cell Line, Tumor; Dipeptides; Female; Humans; Indoles; Inhibitor of Apoptosis Proteins; Mice; Mice, Inbred NOD; Mice, SCID; Mitochondrial Proteins; Oligopeptides; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Precursor Cells, B-Lymphoid; Receptors, Tumor Necrosis Factor, Type I; Thiazoles; Xenograft Model Antitumor Assays

2020
Myeloid Cell-Targeted Nanocarriers Efficiently Inhibit Cellular Inhibitor of Apoptosis for Cancer Immunotherapy.
    Cell chemical biology, 2020, 01-16, Volume: 27, Issue:1

    Topics: Alkynes; Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Colonic Neoplasms; Dendritic Cells; Drug Carriers; Drug Evaluation, Preclinical; Immunotherapy; Interleukin-12; Mice; Myeloid Cells; Nanoparticles; Oligopeptides; Small Molecule Libraries; Thiazoles

2020
Tumor necrosis factor‑related apoptosis‑inducing ligand as a therapeutic option in urothelial cancer cells with acquired resistance against first‑line chemotherapy.
    Oncology reports, 2020, Volume: 43, Issue:4

    Topics: Apoptosis; Baculoviral IAP Repeat-Containing 3 Protein; Caspase 3; Caspase Inhibitors; Cell Line, Tumor; Cisplatin; Deoxycytidine; Gemcitabine; Gene Expression Regulation, Neoplastic; Humans; Inhibitor of Apoptosis Proteins; Signal Transduction; Thiazoles; TNF-Related Apoptosis-Inducing Ligand; Urinary Bladder Neoplasms; Urothelium; X-Linked Inhibitor of Apoptosis Protein

2020
Proteomic Level Changes on Treatment in MCF-7/DDP Breast Cancer Drug- Resistant Cells.
    Anti-cancer agents in medicinal chemistry, 2020, Volume: 20, Issue:6

    Topics: Antineoplastic Agents; Apoptosis; Breast Neoplasms; Caspase Inhibitors; Cell Line, Tumor; Drug Resistance, Neoplasm; Female; Humans; MCF-7 Cells; Proteomics; Signal Transduction; Thiazoles

2020
Targeting the Extrinsic Pathway of Hepatocyte Apoptosis Promotes Clearance of Plasmodium Liver Infection.
    Cell reports, 2020, 03-31, Volume: 30, Issue:13

    Topics: Administration, Oral; Animals; Apoptosis; Biological Availability; Caspase 3; Culicidae; Dipeptides; Hepatocytes; Immunity; Indoles; Inhibitor of Apoptosis Proteins; Life Cycle Stages; Liver; Malaria; Plasmodium; Protozoan Proteins; Sporozoites; Thiazoles; Tumor Necrosis Factor-alpha

2020
The SMAC mimetic LCL161 is a direct ABCB1/MDR1-ATPase activity modulator and BIRC5/Survivin expression down-regulator in cancer cells.
    Toxicology and applied pharmacology, 2020, 08-15, Volume: 401

    Topics: Adenosine Triphosphatases; Antineoplastic Agents; Apoptosis Regulatory Proteins; ATP Binding Cassette Transporter, Subfamily B; Biomimetic Materials; Cell Survival; Dose-Response Relationship, Drug; Down-Regulation; Gene Expression Regulation, Neoplastic; Humans; MCF-7 Cells; Mitochondrial Proteins; Protein Structure, Secondary; Survivin; Thiazoles

2020
In vitro analysis reveals necroptotic signaling does not provoke DNA damage or HPRT mutations.
    Cell death & disease, 2020, 08-13, Volume: 11, Issue:8

    Topics: Animals; Caspases; Cell Death; Cell Line; DNA Damage; Humans; Hypoxanthine Phosphoribosyltransferase; Mice; Mutagenesis; Mutation; Necroptosis; Protein Kinases; Receptor-Interacting Protein Serine-Threonine Kinases; Serpins; Signal Transduction; Thiazoles; Tumor Necrosis Factor-alpha; U937 Cells; Viral Proteins

2020
Combined the SMAC mimetic and BCL2 inhibitor sensitizes neoadjuvant chemotherapy by targeting necrosome complexes in tyrosine aminoacyl-tRNA synthase-positive breast cancer.
    Breast cancer research : BCR, 2020, 11-25, Volume: 22, Issue:1

    Topics: Aniline Compounds; Antineoplastic Combined Chemotherapy Protocols; Apoptosis Regulatory Proteins; Biopsy; Breast; Breast Neoplasms; Carcinoma, Ductal, Breast; Cell Line, Tumor; Clinical Decision-Making; Drug Synergism; Female; Humans; Mastectomy; Mitochondrial Proteins; Necroptosis; Neoadjuvant Therapy; Proto-Oncogene Proteins c-bcl-2; Sulfonamides; Thiazoles; Tyrosine-tRNA Ligase

2020
Induction of interferon-β and interferon signaling by TRAIL and Smac mimetics via caspase-8 in breast cancer cells.
    PloS one, 2021, Volume: 16, Issue:3

    Topics: Antineoplastic Agents; Apoptosis; Apoptosis Regulatory Proteins; Breast Neoplasms; Caspase 8; Cell Line, Tumor; Female; Humans; Interferon-beta; MCF-7 Cells; Mitochondrial Proteins; Signal Transduction; Thiazoles; TNF-Related Apoptosis-Inducing Ligand

2021
Clinical stage drugs targeting inhibitor of apoptosis proteins purge episomal Hepatitis B viral genome in preclinical models.
    Cell death & disease, 2021, 06-23, Volume: 12, Issue:7

    Topics: Animals; Antiviral Agents; Azocines; Benzhydryl Compounds; Disease Models, Animal; Genome, Viral; Hep G2 Cells; Hepatitis B; Hepatitis B virus; Hepatocytes; Host-Pathogen Interactions; Humans; Inhibitor of Apoptosis Proteins; Liver; Mice, Inbred C57BL; Mice, Knockout; Molecular Targeted Therapy; Organoids; Thiazoles; Tumor Necrosis Factor-alpha; Virus Replication

2021
Macrophage and neutrophil death programs differentially confer resistance to tuberculosis.
    Immunity, 2021, 08-10, Volume: 54, Issue:8

    Topics: Animals; Apoptosis; Caspase 8; Cell Line; Dipeptides; Humans; Indoles; Lymphocyte Activation; Macrophages; Mice; Mice, Inbred C57BL; Mice, Knockout; Mycobacterium tuberculosis; Neutrophils; Protein Kinases; Proto-Oncogene Proteins c-bcl-2; T-Lymphocytes; Thiazoles; Tuberculosis, Pulmonary

2021
The smac mimetic LCL161 targets established pulmonary osteosarcoma metastases in mice.
    Clinical & experimental metastasis, 2021, Volume: 38, Issue:5

    Topics: Animals; Antineoplastic Agents; Bone Neoplasms; Cell Line, Tumor; Humans; Lung Neoplasms; Mice; Mice, Inbred BALB C; Osteosarcoma; Thiazoles; Xenograft Model Antitumor Assays

2021
Peptide Stapling Improves the Sustainability of a Peptide-Based Chimeric Molecule That Induces Targeted Protein Degradation.
    International journal of molecular sciences, 2021, Aug-16, Volume: 22, Issue:16

    Topics: Cell-Penetrating Peptides; Estrogen Receptor alpha; Humans; MCF-7 Cells; Protein Binding; Thiazoles; Ubiquitin-Protein Ligases; Ubiquitination

2021
Increased sensitivity to SMAC mimetic LCL161 identified by longitudinal ex vivo pharmacogenomics of recurrent, KRAS mutated rectal cancer liver metastases.
    Journal of translational medicine, 2021, 09-08, Volume: 19, Issue:1

    Topics: Humans; Liver Neoplasms; Pharmacogenetics; Proto-Oncogene Proteins p21(ras); Rectal Neoplasms; Thiazoles

2021
The CXCL Family Contributes to Immunosuppressive Microenvironment in Gliomas and Assists in Gliomas Chemotherapy.
    Frontiers in immunology, 2021, Volume: 12

    Topics: Antineoplastic Agents; Brain Neoplasms; Chemokines, CXC; Clinical Decision-Making; Databases, Chemical; Databases, Genetic; Gene Expression Profiling; Glioma; Humans; Nomograms; Predictive Value of Tests; Prognosis; Risk Assessment; Risk Factors; Thiazoles; Transcriptome; Tumor Microenvironment

2021
Molecular basis for nuclear accumulation and targeting of the inhibitor of apoptosis BIRC2.
    Nature structural & molecular biology, 2023, Volume: 30, Issue:9

    Topics: Apoptosis; Humans; Inhibitor of Apoptosis Proteins; Signal Transduction; Thiazoles; Ubiquitin-Protein Ligases

2023