Results 61 to 70 of about 113,548 (277)

Entinostat-Bortezomib Hybrids against Multiple Myeloma

Molecules, 2023
Although proteasome inhibitors have emerged as the therapeutic backbone of multiple myeloma treatment, patients often relapse and become drug refractory. The combination between proteasome and histone deacetylase inhibitors has shown to be more efficient
Angelica Ferro, Dafni Graikioti, Emre Gezer, Constantinos M. Athanassopoulos, Muriel Cuendet   +4 more
doaj   +1 more source

Identification of a novel polyprenylated acylphloroglucinol‑derived SIRT1 inhibitor with cancer‑specific anti-proliferative and invasion-suppressing activities [PDF]

, 2014
SIRT1, a class III histone deacetylase, plays a critical role in regulating cancer cell growth, migration and invasion, which makes it a potential target for cancer therapeutics.
Chiao, Christine Ya-Chi, Dai, Yan, Faller, Douglas V., Porco, John A., Qi, Ji, Zhang, Qiang, Zhu, Lijia   +6 more
core   +2 more sources

Inhibitors of Histone Deacetylases [PDF]

Journal of Biological Chemistry, 2011
Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.
Kelly Huber, Geneviève Doyon, Joseph Plaks, Elizabeth Fyne, John W. Mellors, Nicolas Sluis-Cremer   +5 more
openaire   +1 more source

Class IIa HDACs forced degradation allows resensitization of oxaliplatin‐resistant FBXW7‐mutated colorectal cancer

Molecular Oncology, EarlyView.
HDAC4 is degraded by the E3 ligase FBXW7. In colorectal cancer, FBXW7 mutations prevent HDAC4 degradation, leading to oxaliplatin resistance. Forced degradation of HDAC4 using a PROTAC compound restores drug sensitivity by resetting the super‐enhancer landscape, reprogramming the epigenetic state of FBXW7‐mutated cells to resemble oxaliplatin ...
Vanessa Tolotto, Nicolò Gualandi, Ylenia Cortolezzis, Raffaella Picco, Monica Colitti, Francesca D'Este, Mariachiara Gani, Wayne W. Hancock, Giovanni Terrosu, Cristina Degrassi, Francesca Agostini, Claudio Brancolini, Luigi E. Xodo, Eros Di Giorgio   +13 more
wiley   +1 more source

Potential of histone deacetylase inhibitors for the therapy of ovarian cancer

Frontiers in Oncology, 2022
Malignant ovarian tumors bear the highest mortality rate among all gynecological cancers. Both late tumor diagnosis and tolerance to available chemotherapy increase patient mortality.
Fengyi Guo, Hongjing Wang, Hongjing Wang
doaj   +1 more source

Activation of AMP-activated protein kinase by metformin induces protein acetylation in prostate and ovarian cancer cells [PDF]

, 2016
AMP-activated protein kinase (AMPK) is an energy sensor and master regulator of metabolism. AMPK functions as a fuel gauge monitoring systemic and cellular energy status.
Galdieri, Luciano, Gatla, Himavanth, Vancura, Ales, Vancurova, Ivana   +3 more
core   +2 more sources

Histone Deacetylase Inhibitors from Burkholderia thailandensis [PDF]

Journal of Natural Products, 2011
Bioactivity-guided fractionation of an extract of Burkholderia thailandensis led to the isolation and identification of a new cytotoxic depsipeptide and its dimer. Both compounds potently inhibited the function of histone deacetylases 1 and 4. The monomer, spiruchostatin C (2), was tested side by side with the clinical depsipeptide FK228 (1, Istodax,
Paul, Klausmeyer, Suzanne M, Shipley, Karina M, Zuck, Thomas G, McCloud   +3 more
openaire   +2 more sources

ATF4‐mediated stress response as a therapeutic vulnerability in chordoma

Molecular Oncology, EarlyView.
We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone, James Dunford, Eleanor Calcutt, Vicki Gamble, Filiz Senbabaoglu Aksu, Lorena Ligammari, Georgina Wherry, Giorgia Gaeta, John C. Christianson, Adrienne M. Flanagan, Udo Oppermann, Adam P. Cribbs   +11 more
wiley   +1 more source

Histone deacetylase inhibitor valproic acid promotes the differentiation of human induced pluripotent stem cells into hepatocyte-like cells. [PDF]

PLoS ONE, 2014
In this study, we aimed to elucidate the effects and mechanism of action of valproic acid on hepatic differentiation from human induced pluripotent stem cell-derived hepatic progenitor cells.
Yuki Kondo, Takahiro Iwao, Sachimi Yoshihashi, Kayo Mimori, Ruri Ogihara, Kiyoshi Nagata, Kouichi Kurose, Masayoshi Saito, Takuro Niwa, Takayoshi Suzuki, Naoki Miyata, Shigeru Ohmori, Katsunori Nakamura, Tamihide Matsunaga   +13 more
doaj   +1 more source

Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells [PDF]

, 2016
Cancer stem cells (CSCs) play an important role in tumor initiation, progression, therapeutic failure and tumor relapse. In this study, we evaluated the efficacy of the thiazole derivative 3-methylcyclopentylidene-[4-(4’-chlorophenyl)thiazol-2-yl ...
Buglioni, Simonetta, Carradori, Simone, DE LUCA, Teresa, De Maria, Ruggero, Del Bufalo, Donatella, Desideri, Marianna, DI MARTILE, Marta, Eramo, Adriana, Gabellini, Chiara, Mai, Antonello, Milella, MICHELE STANISLAW, Rotili, Dante, Secci, Daniela, Sette, Giovanni, Trisciuoglio, Daniela   +14 more
core   +4 more sources