Page last updated: 2024-08-21

pyrazines and lgk974

pyrazines has been researched along with lgk974 in 37 studies

Research

Studies (37)

Timeframe	Studies, this research(%)	All Research%
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	24 (64.86)	24.3611
2020's	13 (35.14)	2.80

Authors

Authors	Studies
Boral, AL; Brenner, JC; Carey, TE; Che, J; Cheng, D; Cheng, J; Flynn, S; Graham, MP; Guo, G; Harris, JL; Hsieh, MH; Kasibhatla, S; Kowal, C; Li, AG; Li, C; Li, J; Liu, J; McLaughlin, ME; McNamara, P; Ng, N; Pan, S; Petruzzelli, L; Pferdekamper, A; Phung, V; Schuller, AG; Schultz, PG; Seidel, HM; Sellers, WR; Steffy, A; Sun, F; Tompkins, C; Vanasse, G; Villarroel, MC; Wang, T; Wang, Y; Wu, X	1
Chen, K; Gaur, S; Hu, S; Liu, YR; Pan, SL; Tzeng, HE; Wang, Y; Yang, L; Yen, Y	1
Eberhart, CG; Hayashi, M; Kahlert, UD; Koch, K; Maciaczyk, J; Natsumeda, M; Orr, BA; Suwala, AK	1
Dong, Y; He, S; Hu, Z; Li, J; Li, K; Luo, L; Ma, H; Sun, Z; Wu, Y; Xu, Z; Zhang, H; Zhang, X; Zheng, J	1
Baryawno, N; Calero, R; Darabi, A; Dyberg, C; Einvik, C; Johnsen, JI; Kogner, P; Kool, M; Milosevic, J; Sandén, E; Siesjö, P; Sveinbjörnsson, B; Wickström, M	1
Balk, SP; Cai, C; Chen, S; Gerrin, SJ; He, HH; He, L; Ma, F; Sowalsky, AG; Tanenbaum, BA; Wang, H; Ye, H; Yuan, X	1
Lum, L; Zhang, LS	2
Acquaviva, A; Bardelli, A; Centonze, A; Crisafulli, G; Medico, E; Novara, L; Petti, C; Picco, G; Torchiaro, E	1
Jang, J; Jho, EH; Jung, Y; Kim, Y; Yoon, Y	1
Amatruda, JF; Bao, X; Bassel-Duby, R; Feng, JQ; Liu, Y; Lum, L; Moon, J; Morlock, LK; Olson, EN; Palecek, SP; Tan, W; Williams, NS; Zhang, LS; Zhang, S; Zhou, H	1
Chen, D; Fan, F; Liu, Q; Shi, Y; Tian, D	1
Dow, LE; Elemento, O; Han, T; Murphy, C; Schatoff, EM; Wilkinson, JE; Zafra, MP	1
Fan, S; Li, A; Li, Y; Liang, C; Meng, J; Shen, X; Wu, D; Wu, G; Xiao, Q; Xu, Y; Zhang, L; Zhang, X	1
Bruens, L; Cammareri, P; Campbell, AD; Faller, WJ; Gay, DM; Hodder, MC; Huels, DJ; McLaughlin, ME; Morrissey, E; Nixon, C; Ridgway, RA; Sansom, OJ; Snippert, HJ; Solar-Abboud, M; van Rheenen, J; Winton, DJ; Zeiger, LB	1
Basler, K; Cantù, C; Cecconi, V; Hafner, J; Hausmann, G; Restivo, G; Valenta, T; van den Broek, M; Zimmerli, D	1
Brommage, R; Cohen-Solal, M; Funck-Brentano, T; Henning, P; Koskela, A; Lerner, UH; Movérare-Skrtic, S; Nilsson, KH; Ohlsson, C; Tuukkanen, J	1
Cheng, JJ; Chiou, CT; Huang, CL; Huang, HM; Huang, HT; Huang, NK; Lee, YC; Yang, JM; Yang, YC	1
Chung, A; Guimaraes, PPG; Jacks, T; Langer, R; Mitchell, MJ; Oberli, M; Riley, RS; Spektor, R; Tammela, T; Tan, M; Viana, CTR; Wang, K; Wu, K	1
Gong, JP; Hu, H; Hu, YB; Li, XL; Mi, YL; Mu, L; Qin, JC; Tao, DD; Wu, YQ; Yan, C; Zhao, H	1
Fang, J; Hao, J; Li, Z; Lian, X; Qin, T; Wu, H; Wu, J; Wu, S; Zhang, W; Zhou, Q	1
Resham, K; Sharma, SS	2
Bagheri, M; Ghasemi, F; Mirzaei, H; Tabatabae Far, MA	1
Chen, H; Fang, J; Jiang, S; Ruan, Q; Sun, J; Yang, X; Zhang, M; Zhang, Y; Zhou, F; Zhou, W; Zhu, T	1
Chen, Y; Li, J; Ruan, N; Wu, G; Xia, Q; Xu, Y; Zhang, Q	1
Chen, S; Liu, S; Wen, F; Xu, H; Yi, M; Yuan, X	1
Ang, GCK; Chang, KT; Guccione, E; Hebrard, M; Lee, VK; Leung, JY; Lim, HJ; Pal, A; Pignata, L; Rao, VK; Taneja, R	1
Panchal, S; Patel, B; Shah, K	1
Jang, J; Jho, EH; Kwon, YV; Lee, H; Sim, I; Song, J; Yoon, Y	1
Albany, C; Chovanec, M; Cierna, Z; Kalavska, K; Konig, H; Kucerova, L; Liskova, V; Matuskova, M; Mego, M; Miklikova, S; Plava, J; Rogozea, A; Rojikova, L; Schmidtova, S	1
Argilés, G; Connolly, RM; de Jonge, M; Dobson, JR; Garralda, E; Giannakis, M; Janku, F; Ji, Y; McLaughlin, ME; Moody, SE; Morawiak, J; Rodon, J; Seroutou, A; Smith, DC; Vaishampayan, U	1
Arasaki, A; Kawabata-Iwakawa, R; Kina, S; Kinjo, T; Miyamoto, S; Sunakawa, H	1
Bian, Z; Chen, M; Gong, RH; Huang, C; Kwan, HY; Wong, HLX	1
Darabi, M; Hosseini, V; Kalantary-Charvadeh, A; Mehdizadeh, A; Nazari Soltan Ahmad, S; Nouri, M; Nozad Charoudeh, H; Rahbarghazi, R	1
Huang, PH; Ji, Y; Myers, A; Woolfenden, S	1
Donnelly, L; Elghobashi-Meinhardt, N; Li, X; Liu, Y; Long, T; Qi, X; Sun, Y; Wang, B; Zhou, RW	1

Reviews

2 review(s) available for pyrazines and lgk974

Article	Year
Chemical Modulation of WNT Signaling in Cancer. Progress in molecular biology and translational science, 2018, Volume: 153 Topics: Acyltransferases; Humans; Membrane Proteins; Neoplasms; Pyrazines; Pyridines; Wnt Proteins; Wnt Signaling Pathway	2018
Porcupine inhibitors: Novel and emerging anti-cancer therapeutics targeting the Wnt signaling pathway. Pharmacological research, 2021, Volume: 167 Topics: Acyltransferases; Animals; Antineoplastic Agents; Drug Development; Drug Discovery; Enzyme Inhibitors; Humans; Membrane Proteins; Molecular Targeted Therapy; Neoplasms; Pyrazines; Pyridines; Wnt Signaling Pathway	2021

Trials

1 trial(s) available for pyrazines and lgk974

Article	Year
Phase 1 study of single-agent WNT974, a first-in-class Porcupine inhibitor, in patients with advanced solid tumours. British journal of cancer, 2021, Volume: 125, Issue:1 Topics: Administration, Oral; Adult; Aged; Axin Protein; Enzyme Inhibitors; Female; Gene Expression Regulation, Neoplastic; Humans; Male; Middle Aged; Neoplasms; Pyrazines; Pyridines; Treatment Outcome; Wnt Signaling Pathway	2021

Other Studies

34 other study(ies) available for pyrazines and lgk974

Article	Year
Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proceedings of the National Academy of Sciences of the United States of America, 2013, Dec-10, Volume: 110, Issue:50 Topics: Acyltransferases; Animals; Axin Protein; Blotting, Western; Cell Line, Tumor; Cloning, Molecular; High-Throughput Screening Assays; Humans; Membrane Proteins; Mice; Mutagenesis; Neoplasms; Phosphorylation; Pyrazines; Pyridines; Radioligand Assay; Rats; Receptors, Notch; Reverse Transcriptase Polymerase Chain Reaction; Wnt Signaling Pathway	2013
The pan-PI3K inhibitor GDC-0941 activates canonical WNT signaling to confer resistance in TNBC cells: resistance reversal with WNT inhibitor. Oncotarget, 2015, May-10, Volume: 6, Issue:13 Topics: Animals; Apoptosis; beta Catenin; Blotting, Western; Cell Proliferation; Drug Resistance, Neoplasm; Female; Fluorescent Antibody Technique; Humans; Indazoles; Mice; Mice, Nude; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazines; Pyridines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sulfonamides; TOR Serine-Threonine Kinases; Triple Negative Breast Neoplasms; Tumor Cells, Cultured; Wnt Proteins; Xenograft Model Antitumor Assays	2015
Pharmacologic Wnt Inhibition Reduces Proliferation, Survival, and Clonogenicity of Glioblastoma Cells. Journal of neuropathology and experimental neurology, 2015, Volume: 74, Issue:9 Topics: Adult; Brain Neoplasms; Cell Line, Tumor; Cell Proliferation; Cell Survival; Child; Glioblastoma; Humans; Pyrazines; Pyridines; Tumor Stem Cell Assay; Wnt Signaling Pathway	2015
Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors. Bioorganic & medicinal chemistry, 2015, Nov-01, Volume: 23, Issue:21 Topics: Acyltransferases; Animals; Cytochrome P-450 CYP3A; Drug Design; Genes, Reporter; HEK293 Cells; Humans; Membrane Proteins; Microsomes, Liver; Pyrazines; Pyridines; Rats; Structure-Activity Relationship; Wnt Signaling Pathway	2015
Wnt/β-catenin pathway regulates MGMT gene expression in cancer and inhibition of Wnt signalling prevents chemoresistance. Nature communications, 2015, Nov-25, Volume: 6 Topics: Animals; Antineoplastic Agents; Benzeneacetamides; beta Catenin; Brain Neoplasms; Camptothecin; Celecoxib; Cisplatin; Colorectal Neoplasms; Dacarbazine; DNA Modification Methylases; DNA Repair Enzymes; Doxorubicin; Drug Resistance, Neoplasm; Flow Cytometry; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Glioma; Glucose-6-Phosphate Isomerase; Heterocyclic Compounds, 3-Ring; Humans; Immunoblotting; Immunohistochemistry; Irinotecan; Medulloblastoma; Mice; Neoplasm Transplantation; Neoplasms; Neuroblastoma; Pyrans; Pyrazines; Pyridines; Real-Time Polymerase Chain Reaction; Sulfones; Temozolomide; Triazoles; Tumor Suppressor Proteins; Vincristine; Wnt Proteins; Wnt Signaling Pathway	2015
SOX9 drives WNT pathway activation in prostate cancer. The Journal of clinical investigation, 2016, 05-02, Volume: 126, Issue:5 Topics: Animals; Basic Helix-Loop-Helix Leucine Zipper Transcription Factors; Cell Line, Tumor; Gene Expression Regulation, Neoplastic; Humans; Male; Mice; Mice, Nude; Mice, SCID; Neoplasm Proteins; Prostatic Neoplasms; Pyrazines; Pyridines; SOX9 Transcription Factor; Transcription Factor 4; Transcription Factors; Wnt Signaling Pathway; Xenograft Model Antitumor Assays	2016
Delivery of the Porcupine Inhibitor WNT974 in Mice. Methods in molecular biology (Clifton, N.J.), 2016, Volume: 1481 Topics: Acyltransferases; Animals; Membrane Proteins; Mice; Molecular Biology; Pyrazines; Pyridines; Wnt Proteins; Wnt Signaling Pathway	2016
Loss of AXIN1 drives acquired resistance to WNT pathway blockade in colorectal cancer cells carrying RSPO3 fusions. EMBO molecular medicine, 2017, Volume: 9, Issue:3 Topics: Axin Protein; Cell Line, Tumor; Cell Proliferation; Colorectal Neoplasms; Drug Resistance; Enzyme Inhibitors; Gene Fusion; Humans; Pyrazines; Pyridines; Thrombospondins; Wnt Proteins; Wnt Signaling Pathway	2017
LPS-induced inflammatory response is suppressed by Wnt inhibitors, Dickkopf-1 and LGK974. Scientific reports, 2017, 01-27, Volume: 7 Topics: Anti-Inflammatory Agents; Cell Line; Cytokines; Epithelial Cells; Gene Expression Regulation; Gene Knockdown Techniques; Humans; Inflammation; Inflammation Mediators; Intercellular Signaling Peptides and Proteins; Lipopolysaccharides; NF-kappa B; Protein Binding; Pyrazines; Pyridines; Wnt Proteins; Wnt Signaling Pathway	2017
Blockade to pathological remodeling of infarcted heart tissue using a porcupine antagonist. Proceedings of the National Academy of Sciences of the United States of America, 2017, 02-14, Volume: 114, Issue:7 Topics: Acyltransferases; Animals; Atrial Remodeling; Cells, Cultured; Collagen Type VI; Enzyme Inhibitors; Gene Expression; HEK293 Cells; Humans; Membrane Proteins; Mice, Inbred C57BL; Molecular Structure; Myocardial Infarction; Pyrazines; Pyridines; Regeneration; Wnt Signaling Pathway	2017
The Wnt inhibitor LGK-974 enhances radiosensitivity of HepG2 cells by modulating Nrf2 signaling. International journal of oncology, 2017, Volume: 51, Issue:2 Topics: Acyltransferases; Apoptosis; Endoplasmic Reticulum; Hep G2 Cells; Humans; Liver Neoplasms; Membrane Proteins; NF-E2-Related Factor 2; Pyrazines; Pyridines; Radiation Tolerance; Reactive Oxygen Species; Signal Transduction; Wnt Signaling Pathway; Wnt3A Protein	2017
R-Spondin chromosome rearrangements drive Wnt-dependent tumour initiation and maintenance in the intestine. Nature communications, 2017, 07-11, Volume: 8 Topics: Acyltransferases; Animals; Chromosome Aberrations; Chromosomes; Colonic Neoplasms; Female; Gene Rearrangement; Humans; Intestines; Male; Membrane Proteins; Mice; Mice, Inbred C57BL; Pyrazines; Pyridines; Receptor-Like Protein Tyrosine Phosphatases, Class 2; Thrombospondins; Wnt Proteins	2017
Canonical Wnt inhibitors ameliorate cystogenesis in a mouse ortholog of human ADPKD. JCI insight, 2018, 03-08, Volume: 3, Issue:5 Topics: Animals; beta Catenin; Disease Models, Animal; Female; Heterocyclic Compounds, 3-Ring; Humans; Injections, Intraperitoneal; Kidney; Male; Mice; Mice, Inbred C57BL; Mice, Transgenic; Mutation; Polycystic Kidney, Autosomal Dominant; Pyrazines; Pyridines; Random Allocation; Survival Analysis; Treatment Outcome; TRPP Cation Channels; Wnt Signaling Pathway	2018
Wnt ligands influence tumour initiation by controlling the number of intestinal stem cells. Nature communications, 2018, 03-19, Volume: 9, Issue:1 Topics: Acyltransferases; Adenoma; Adenomatous Polyposis Coli Protein; Animals; Carcinogenesis; Cell Transformation, Neoplastic; Colorectal Neoplasms; Enzyme Inhibitors; Intestinal Mucosa; Ligands; Membrane Proteins; Mice; Mice, Inbred C57BL; Mice, Transgenic; Pyrazines; Pyridines; Stem Cells; Wnt Signaling Pathway	2018
WNT ligands control initiation and progression of human papillomavirus-driven squamous cell carcinoma. Oncogene, 2018, Volume: 37, Issue:27 Topics: Acyltransferases; Animals; Carcinoma, Squamous Cell; Enzyme Inhibitors; Gene Expression Profiling; Humans; Membrane Proteins; Mice; Neoplastic Stem Cells; Papillomaviridae; Papillomavirus Infections; Pyrazines; Pyridines; Skin Neoplasms; Stem Cell Niche; Wnt Proteins; Wnt Signaling Pathway	2018
Porcupine inhibitors impair trabecular and cortical bone mass and strength in mice. The Journal of endocrinology, 2018, Volume: 238, Issue:1 Topics: Acyltransferases; Animals; Animals, Newborn; Bone and Bones; Bone Density; Cells, Cultured; Cortical Bone; Female; Femur; Flexural Strength; Membrane Proteins; Mice; Mice, Inbred C57BL; Osteoblasts; Pyrazines; Pyridines; Stress, Mechanical; Tibia	2018
LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway. Toxicology, 2018, 12-01, Volume: 410 Topics: Antineoplastic Agents; Apoptosis; Apoptosis Regulatory Proteins; beta Catenin; Cell Line; Cell Line, Tumor; Cell Survival; Glycogen Synthase Kinase 3; Humans; Immunohistochemistry; Paraquat; Parkinson Disease; Pyrazines; Pyridines; Wnt Signaling Pathway	2018
Potent in vivo lung cancer Wnt signaling inhibition via cyclodextrin-LGK974 inclusion complexes. Journal of controlled release : official journal of the Controlled Release Society, 2018, 11-28, Volume: 290 Topics: Adenocarcinoma of Lung; Animals; Antineoplastic Agents; Cell Line, Tumor; Cyclodextrins; Humans; Lung Neoplasms; Mice, Nude; Pyrazines; Pyridines; Wnt Proteins; Wnt Signaling Pathway	2018
Exosomal Wnt-induced dedifferentiation of colorectal cancer cells contributes to chemotherapy resistance. Oncogene, 2019, Volume: 38, Issue:11 Topics: Animals; Antineoplastic Agents; Cell Dedifferentiation; Cell Proliferation; Cells, Cultured; Colorectal Neoplasms; Drug Resistance, Neoplasm; Exosomes; Female; Fibroblasts; Fluorouracil; HT29 Cells; Humans; Mice; Mice, Inbred NOD; Mice, SCID; Neoplastic Stem Cells; Oxaliplatin; Paracrine Communication; Pyrazines; Pyridines; Wnt Signaling Pathway; Xenograft Model Antitumor Assays	2019
Discovery and structure-activity relationship study of phthalimide-phenylpyridine conjugate as inhibitor of Wnt pathway. Bioorganic & medicinal chemistry letters, 2019, 04-01, Volume: 29, Issue:7 Topics: Bridged Bicyclo Compounds, Heterocyclic; Molecular Structure; Pyrazines; Pyridines; Pyrimidinones; Signal Transduction; Structure-Activity Relationship; Wnt Signaling Pathway	2019
Pharmacologic Inhibition of Porcupine, Disheveled, and β-Catenin in Wnt Signaling Pathway Ameliorates Diabetic Peripheral Neuropathy in Rats. The journal of pain, 2019, Volume: 20, Issue:11 Topics: Animals; beta Catenin; Depsipeptides; Diabetes Mellitus, Experimental; Diabetic Neuropathies; Dishevelled Proteins; Enzyme Inhibitors; Male; Pyrazines; Pyridines; Rats; Rats, Sprague-Dawley; Wnt Signaling Pathway	2019
Evaluation of antitumor effects of aspirin and LGK974 drugs on cellular signaling pathways, cell cycle and apoptosis in colorectal cancer cell lines compared to oxaliplatin drug. Fundamental & clinical pharmacology, 2020, Volume: 34, Issue:1 Topics: Antineoplastic Agents; Apoptosis; Aspirin; Cell Cycle; Cell Line, Tumor; Colorectal Neoplasms; Gene Expression Regulation, Neoplastic; Humans; Inhibitory Concentration 50; MAP Kinase Signaling System; Oxaliplatin; Pyrazines; Pyridines; Wnt Signaling Pathway	2020
WNT5B governs the phenotype of basal-like breast cancer by activating WNT signaling. Cell communication and signaling : CCS, 2019, 08-28, Volume: 17, Issue:1 Topics: Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Female; Humans; Phenotype; Pyrazines; Pyridines; Wnt Proteins; Wnt Signaling Pathway	2019
Pharmacological interventions targeting Wnt/β-catenin signaling pathway attenuate paclitaxel-induced peripheral neuropathy. European journal of pharmacology, 2019, Dec-01, Volume: 864 Topics: Animals; Behavior, Animal; Depsipeptides; Gene Expression Regulation; Male; Paclitaxel; Peripheral Nervous System Diseases; Pyrazines; Pyridines; Rats; Rats, Sprague-Dawley; Sciatic Nerve; Wnt Signaling Pathway	2019
Porcupine Inhibitor LGK974 Downregulates the Wnt Signaling Pathway and Inhibits Clear Cell Renal Cell Carcinoma. BioMed research international, 2020, Volume: 2020 Topics: Acyltransferases; Carcinoma, Renal Cell; Cell Line, Tumor; Down-Regulation; Gene Expression Regulation, Neoplastic; Humans; Kidney Neoplasms; Membrane Proteins; Neoplasm Proteins; Pyrazines; Pyridines; Wnt Signaling Pathway	2020
WNT974 Inhibits Proliferation, Induces Apoptosis, and Enhances Chemosensitivity to Doxorubicin in Lymphoma Cells by Inhibiting Wnt/β-Catenin Signaling. Medical science monitor : international medical journal of experimental and clinical research, 2020, Jun-29, Volume: 26 Topics: Apoptosis; Cell Line, Tumor; Cell Proliferation; Doxorubicin; Drug Resistance, Neoplasm; Enzyme Inhibitors; Humans; Lymphoma; Pyrazines; Pyridines; Wnt Signaling Pathway	2020
EHMT2 epigenetically suppresses Wnt signaling and is a potential target in embryonal rhabdomyosarcoma. eLife, 2020, 11-30, Volume: 9 Topics: Animals; Cell Differentiation; Cell Line, Tumor; Cell Proliferation; Dimethyl Sulfoxide; Epigenesis, Genetic; Gene Expression Regulation, Developmental; Gene Expression Regulation, Neoplastic; Genetic Predisposition to Disease; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Mice; Mice, Nude; Puromycin; Pyrazines; Pyridines; Quinazolines; Rhabdomyosarcoma, Embryonal; RNA Interference; Wnt Signaling Pathway	2020
LGK974 suppresses lipopolysaccharide-induced endotoxemia in mice by modulating the crosstalk between the Wnt/β-catenin and NF-κB pathways. Experimental & molecular medicine, 2021, Volume: 53, Issue:3 Topics: Animals; beta Catenin; Endotoxemia; Enzyme Inhibitors; Gene Expression Regulation; Humans; Lipopolysaccharides; Male; Mice; Mice, Inbred C57BL; NF-kappa B; Pyrazines; Pyridines; Sepsis; Wnt1 Protein	2021
Targeting of Deregulated Wnt/β-Catenin Signaling by PRI-724 and LGK974 Inhibitors in Germ Cell Tumor Cell Lines. International journal of molecular sciences, 2021, Apr-20, Volume: 22, Issue:8 Topics: Animals; Antineoplastic Agents; Apoptosis; beta Catenin; Bridged Bicyclo Compounds, Heterocyclic; Cell Line, Tumor; Cisplatin; Drug Resistance, Neoplasm; Humans; Immunohistochemistry; Male; Mice; Mice, SCID; Neoplasms, Germ Cell and Embryonal; Pyrazines; Pyridines; Pyrimidinones; Testicular Neoplasms; Wnt Signaling Pathway	2021
A molecular signature of well-differentiated oral squamous cell carcinoma reveals a resistance mechanism to metronomic chemotherapy and novel therapeutic candidates. Journal of drug targeting, 2021, Volume: 29, Issue:10 Topics: Administration, Metronomic; Adult; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Drug Resistance, Neoplasm; Drug Synergism; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Middle Aged; Neoadjuvant Therapy; Pyrazines; Pyridines; Retrospective Studies; Squamous Cell Carcinoma of Head and Neck; Survival Rate; Tongue Neoplasms; Wnt Signaling Pathway; Young Adult	2021
Combination of artesunate and WNT974 induces KRAS protein degradation by upregulating E3 ligase ANACP2 and β-TrCP in the ubiquitin-proteasome pathway. Cell communication and signaling : CCS, 2022, 03-19, Volume: 20, Issue:1 Topics: Animals; Apc2 Subunit, Anaphase-Promoting Complex-Cyclosome; Artesunate; beta-Transducin Repeat-Containing Proteins; Cell Line, Tumor; Cullin Proteins; Glycogen Synthase Kinase 3 beta; Humans; Mice; Phosphatidylinositol 3-Kinases; Proteasome Endopeptidase Complex; Proteolysis; Proto-Oncogene Proteins c-akt; Proto-Oncogene Proteins p21(ras); Pyrazines; Pyridines; TOR Serine-Threonine Kinases; Ubiquitin-Conjugating Enzymes; Ubiquitin-Protein Ligases; Ubiquitins; Wnt Signaling Pathway	2022
The porcupine inhibitor WNT974 provokes ectodermal lineage differentiation of human embryonic stem cells. Cell biochemistry and function, 2022, Volume: 40, Issue:4 Topics: Acyltransferases; Human Embryonic Stem Cells; Humans; Membrane Proteins; Pyrazines; Pyridines; Stearoyl-CoA Desaturase; Wnt Signaling Pathway	2022
Model-based dose selection to inform translational clinical oncology development of WNT974, a first-in-class Porcupine inhibitor. Clinical and translational science, 2022, Volume: 15, Issue:7 Topics: Antineoplastic Agents; Dose-Response Relationship, Drug; Humans; Maximum Tolerated Dose; Neoplasms; Pyrazines; Pyridines; Treatment Outcome	2022
Mechanisms and inhibition of Porcupine-mediated Wnt acylation. Nature, 2022, Volume: 607, Issue:7920 Topics: Acylation; Acyltransferases; Antineoplastic Agents; Binding Sites; Coenzyme A; Cryoelectron Microscopy; Histidine; Humans; Membrane Proteins; Neoplasms; Palmitoyl Coenzyme A; Pyrazines; Pyridines; Serine; Substrate Specificity; Wnt Signaling Pathway; Wnt3A Protein	2022