Hitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3)

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Hitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3) is …
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scholarly articleQ13442814

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P356DOI10.1016/J.MOLONC.2015.02.012
P932PMC publication ID5528765
P698PubMed publication ID25777967

P50authorLaurent PerezQ40036974
Maurizio FermegliaQ41134526
Sabrina PriclQ41134546
Lara BrambillaQ63762414
Giuseppina M CarboneQ90138640
Carlo V CatapanoQ90138646
Erik LauriniQ90653270
Davide GeniniQ117257448
Jessica MerullaQ117257449
P2860cites workPhosphorylation of EZH2 activates STAT3 signaling via STAT3 methylation and promotes tumorigenicity of glioblastoma stem-like cellsQ24293124
Activation of signal transducer and activator of transcription 3 through a phosphomimetic serine 727 promotes prostate tumorigenesis independent of tyrosine 705 phosphorylationQ24632832
Three-dimensional structure of the Stat3beta homodimer bound to DNAQ27764842
STAT3 nuclear import is independent of tyrosine phosphorylation and mediated by importin-alpha3.Q28253106
Structure, function, and regulation of STAT proteinsQ28282800
Maximal activation of transcription by Stat1 and Stat3 requires both tyrosine and serine phosphorylationQ28288257
Requirement of serine phosphorylation for formation of STAT-promoter complexesQ28637366
Stat3: a STAT family member activated by tyrosine phosphorylation in response to epidermal growth factor and interleukin-6Q28637521
STATs in cancer inflammation and immunity: a leading role for STAT3Q29547203
AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibilityQ29547658
Stats: transcriptional control and biological impactQ29547776
Transcriptional and Non-Transcriptional Functions of PPARβ/δ in Non-Small Cell Lung CancerQ31103456
Stattic: a small-molecule inhibitor of STAT3 activation and dimerizationQ33264035
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activityQ33282964
The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumorsQ33613105
Therapeutic modulators of STAT signalling for human diseasesQ33684732
A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cellsQ33935165
Acetylated STAT3 is crucial for methylation of tumor-suppressor gene promoters and inhibition by resveratrol results in demethylation.Q34272080
Stat3 dimerization regulated by reversible acetylation of a single lysine residueQ34384817
Autocrine IL-6 signaling: a key event in tumorigenesis?Q34732166
Oncogene mimicry as a mechanism of primary resistance to BRAF inhibitorsQ34960206
Toward a new STATe: the role of STATs in mitochondrial functionQ35064219
Direct reprogramming of stem cell properties in colon cancer cells by CD44Q35176968
The JAK2/STAT3 signaling pathway is required for growth of CD44⁺CD24⁻ stem cell-like breast cancer cells in human tumorsQ35572396
Unphosphorylated STAT3 accumulates in response to IL-6 and activates transcription by binding to NFkappaBQ35812229
Mechanisms of unphosphorylated STAT3 transcription factor binding to DNA.Q35922290
Targeting the interleukin-6/Jak/stat pathway in human malignanciesQ35925127
Loss of androgen receptor expression promotes a stem-like cell phenotype in prostate cancer through STAT3 signalingQ35963362
Interleukin-6 regulation of prostate cancer cell growthQ36101905
JAK and STAT signaling molecules in immunoregulation and immune-mediated diseaseQ36404704
Molecular approaches towards the inhibition of the signal transducer and activator of transcription 3 (Stat3) proteinQ37015696
Promoter-specific transcriptional interference and c-myc gene silencing by siRNAs in human cellsQ37234973
Paradigm shifts in the cell biology of STAT signalingQ37240242
Targeting signal transducer and activator of transcription signaling pathway in leukemias.Q37347522
Function of mitochondrial Stat3 in cellular respirationQ37378567
Disruption of Stat3 reveals a critical role in both the initiation and the promotion stages of epithelial carcinogenesisQ37486563
Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.Q38014908
Revisiting STAT3 signalling in cancer: new and unexpected biological functionsQ38262473
Constitutive activation of Stat3 in human prostate tumors and cell lines: direct inhibition of Stat3 signaling induces apoptosis of prostate cancer cellsQ38360859
Drug resistance via feedback activation of Stat3 in oncogene-addicted cancer cells.Q38971290
JAK-STAT blockade inhibits tumor initiation and clonogenic recovery of prostate cancer stem-like cellsQ39130848
OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cellsQ39195889
Homology Model and Docking-Based Virtual Screening for Ligands of the σ1 Receptor.Q39508226
Mitochondrial STAT3 supports Ras-dependent oncogenic transformation.Q39675800
Synergistic experimental/computational studies on arylazoenamine derivatives that target the bovine viral diarrhea virus RNA-dependent RNA polymerase.Q39678894
Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cellsQ39899676
Live cell imaging of interleukin-6-induced targeting of "transcription factor" STAT3 to sequestering endosomes in the cytoplasm.Q40099327
Inhibiting Stat3 signaling in the hematopoietic system elicits multicomponent antitumor immunityQ40351340
A novel STAT inhibitor, OPB-31121, has a significant antitumor effect on leukemia with STAT-addictive oncokinasesQ41850042
Another brick in the wall. Validation of the σ1 receptor 3D model by computer-assisted design, synthesis, and activity of new σ1 ligandsQ45108635
Stat3 activation in prostatic carcinomas.Q53390466
Enhancing Chemotherapy Efficacy in Pten -Deficient Prostate Tumors by Activating the Senescence-Associated Antitumor ImmunityQ63884125
The molecular basis of IGF-II/IGF2R recognition: a combined molecular dynamics simulation, free-energy calculation and computational alanine scanning studyQ84563006
Phase 1, open-label, dose-escalation, and pharmacokinetic study of STAT3 inhibitor OPB-31121 in subjects with advanced solid tumorsQ87857581
P433issue6
P304page(s)1194-1206
P577publication date2015-03-05
P1433published inMolecular OncologyQ2190736
P1476titleHitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3)
P478volume9

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cites work (P2860)
Q52671159A First-in-Human Phase 1 Study of OPB-111077, a Small-Molecule STAT3 and Oxidative Phosphorylation Inhibitor, in Patients with Advanced Cancers.
Q38591166A STAT inhibitor patent review: progress since 2011.
Q39275789Cancer stem cell (CSC) inhibitors: a review of recent patents (2012-2015).
Q52655179Effects of purified Omphalia lapidescens protein on metastasis, cell cycle, apoptosis and the JAK-STAT signaling pathway in SGC-7901 human gastric cells.
Q93190592If You Cannot Win Them, Join Them: Understanding New Ways to Target STAT3 by Small Molecules
Q49273540Impact of STAT3 phosphorylation in glioblastoma stem cells radiosensitization and patient outcome
Q47150116Mitochondrial dysfunction induced by a SH2 domain-targeting STAT3 inhibitor leads to metabolic synthetic lethality in cancer cells
Q41347601Molecular and functional characterization of a new 3' end KIT juxtamembrane deletion in a duodenal GIST treated with neoadjuvant Imatinib
Q36343400Multiple regulation pathways and pivotal biological functions of STAT3 in cancer.
Q38870465Novel STAT 3 inhibitors for treating gastric cancer
Q90697887Overview of the STAT-3 signaling pathway in cancer and the development of specific inhibitors
Q26798034Pattern Recognition Receptors in Cancer Progression and Metastasis
Q92814428Pharmacological Inhibition of Oncogenic STAT3 and STAT5 Signaling in Hematopoietic Cancers
Q92735027Protopanaxadiol inhibits epithelial-mesenchymal transition of hepatocellular carcinoma by targeting STAT3 pathway
Q90697892Role and mechanism of programmed death-ligand 1 in hypoxia-induced liver cancer immune escape
Q55637644Structural Biology of STAT3 and Its Implications for Anticancer Therapies Development.
Q90533200Targeted inhibition of STAT3 as a potential treatment strategy for atherosclerosis
Q90540850Targeting Janus Kinases and Signal Transducer and Activator of Transcription 3 to Treat Inflammation, Fibrosis, and Cancer: Rationale, Progress, and Caution
Q89157968Targeting Transcription Factors for Cancer Treatment
Q50191433Targeting the IL-6/JAK/STAT3 signalling axis in cancer
Q38687571The STAT3 pathway as a therapeutic target in head and neck cancer: Barriers and innovations
Q64260465Transcriptional Reprogramming and Novel Therapeutic Approaches for Targeting Prostate Cancer Stem Cells

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