T‐17, a novel cyclin‐dependent kinases/histone deacetylases dual inhibitor, induces cancer cells death through cell cycle arrest and apoptosis
Sign Up to like & getrecommendations! Published in 2022 at "Drug Development Research"
DOI: 10.1002/ddr.21977
Abstract: Combination of cyclin‐dependent kinases (CDKs) and histone deacetylases (HDACs) inhibitors may have statistical synergy in suppressing cancer cell proliferation. Herein, a novel CDKs/HDACs dual inhibitor T‐17 was rationally designed, synthesized, and evaluated. Our results demonstrated… read more here.
Keywords: cell; dual inhibitor; cyclin dependent; histone deacetylases ... See more keywords
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01804
Abstract: Inspired by previously discovered enhanced analgesic efficacy between soluble epoxide hydrolase (sEH) and phosphodiesterase 4 (PDE4) inhibitors, we designed, synthesized and characterized 21 novel sEH/PDE4 dual inhibitors. The best of these displayed good efficacy in… read more here.
Keywords: soluble epoxide; dual inhibitor; epoxide hydrolase; inflammatory pain ... See more keywords
Protoporphyrin IX is a dual inhibitor of p53/MDM2 and p53/MDM4 interactions and induces apoptosis in B-cell chronic lymphocytic leukemia cells
Sign Up to like & getrecommendations! Published in 2019 at "Cell Death Discovery"
DOI: 10.1038/s41420-019-0157-7
Abstract: Abstractp53 is a tumor suppressor, which belongs to the p53 family of proteins. The family consists of p53, p63 and p73 proteins, which share similar structure and function. Activation of wild-type p53 or TAp73 in… read more here.
Keywords: mdm4 interactions; dual inhibitor; inhibitor p53; p53 ... See more keywords
A dual inhibitor of the proteasome catalytic subunits LMP2 and Y attenuates disease progression in mouse models of Alzheimer’s disease
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-54846-z
Abstract: The immunoproteasome (iP) is a variant of the constitutive proteasome (cP) that is abundantly expressed in immune cells which can also be induced in somatic cells by cytokines such as TNF-α or IFN-γ. Accumulating evidence… read more here.
Keywords: alzheimer disease; mouse models; dual inhibitor;
PD10-02 THE MTORC1/2 DUAL INHIBITOR AZD2014 WITH POTENT ANTITUMOR ACTIVITY IN DOCETAXEL SENSITIVE/RESISTANT PROSTATE CANCER IN VITRO
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Urology"
DOI: 10.1097/ju.0000000000000844.02
Abstract: INTRODUCTION AND OBJECTIVE:The mammalian target of rapamycin (mTOR) is a vital effect factor in regulating cell growth, survival and autophagy via direct interaction with mTORC1 (mTOR complex 1) an... read more here.
Keywords: pd10 mtorc1; mtorc1 dual; azd2014 potent; potent antitumor ... See more keywords
Vorasidenib, a Dual Inhibitor of Mutant IDH1/2, in Recurrent or Progressive Glioma; Results of a First-in-Human Phase I Trial
Sign Up to like & getrecommendations! Published in 2021 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-21-0611
Abstract: Purpose: Lower grade gliomas (LGGs) are malignant brain tumors. Current therapy is associated with short- and long-term toxicity. Progression to higher tumor grade is associated with contrast enhancement on MRI. The majority of LGGs harbor… read more here.
Keywords: recurrent progressive; glioma; vorasidenib; mutant idh1 ... See more keywords
Abstract 2754: NT219, a novel dual inhibitor of STAT3 and IRS1/2, converts immuno-oncology resistant tumors to responders
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-2754
Abstract: Feedback activation of STAT3 and IGF1R/IRS plays a prominent role in mediating drug resistance to a broad spectrum of targeted cancer therapies and chemotherapies. Both the IRS1/2 and STAT3 are major signaling junctions regulated by… read more here.
Keywords: dual inhibitor; stat3; irs1; cancer ... See more keywords
Abstract 5269: RF-1302, a novel dual inhibitor of PIM1 and FLT3 in preclinical treatment of acute myeloid leukemia
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-5269
Abstract: It was reported that PIM (Proviral Insertion site in Moloney murine leukemia virus) proteins are family kinases (PIM1, PIM2, and PIM3), which are upregulated in several cancer types, especially PIM1 is highly expressed in hematopoietic… read more here.
Keywords: myeloid leukemia; novel dual; leukemia; dual inhibitor ... See more keywords
Targeting ERK enhances the cytotoxic effect of the novel PI3K and mTOR dual inhibitor VS-5584 in preclinical models of pancreatic cancer
Sign Up to like & getrecommendations! Published in 2017 at "Oncotarget"
DOI: 10.18632/oncotarget.17869
Abstract: Pancreatic ductal adenocarcinoma (PDAC) is a deadly disease in urgent need of newer therapeutic modalities. Majority of patients with PDAC have mutations in KRAS, which unfortunately remains an ineffectual target. Our strategy here is to… read more here.
Keywords: pi3k mtor; inhibitor; dual inhibitor; mtor dual ... See more keywords
COX-2/sEH dual inhibitor PTUPB suppresses glioblastoma growth by targeting epidermal growth factor receptor and hyaluronan mediated motility receptor
Sign Up to like & getrecommendations! Published in 2017 at "Oncotarget"
DOI: 10.18632/oncotarget.20928
Abstract: Aims Cyclooxygenase-2 (COX-2)/soluble epoxide hydrolase (sEH) dual inhibitor, PTUPB, has been demonstrated to inhibit angiogenesis, primary tumor growth and metastasis. The aim of this study is to investigate the effects of PTUPB on glioblastoma cells… read more here.
Keywords: ptupb; cell; dual inhibitor; seh dual ... See more keywords
Novel HSP90-PI3K Dual Inhibitor Suppresses Melanoma Cell Proliferation by Interfering with HSP90-EGFR Interaction and Downstream Signaling Pathways
Sign Up to like & getrecommendations! Published in 2020 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms21051845
Abstract: Melanoma is the deadliest form of skin cancer, and its incidence has continuously increased over the past 20 years. Therefore, the discovery of a novel targeted therapeutic strategy for melanoma is urgently needed. In our… read more here.
Keywords: cell proliferation; pi3k dual; dual inhibitor; hsp90 pi3k ... See more keywords