Results 41 to 50 of about 2,934,766 (329)

Histone deacetylase activity mediates acquired resistance towards structurally diverse HSP90 inhibitors [PDF]

, 2017
Heat shock protein 90 (HSP90) regulates multiple signalling pathways critical for tumour growth. As such, HSP90 inhibitors have been shown to act as effective anticancer agents in preclinical studies but, for a number of reasons, the same effect has not ...
Baker, Brough, Butler, Cercek, Chambers, Chen, Dickson, Eccles, Gaspar, George, Greer, Guo, Heath, Holmes, Jhaveri, Johnson, Kim, Kovacs, Kramer, Liu, Maloney, McCollum, McCollum, Page, Peserico, Price, Rae, Ramalingam, Rao, Rocha Dias, Ronnen, Ross, Sato, Scroggins, Sellappan, Sharp, Skehan, Smith, Solit, Tatokoro, Trepel, Wang, Wang, Wardley, Wei, Whitesell, Whitesell, Xu, Yang, Yong, Younes, Zhang, Zhang, Zupkovitz   +53 more
core   +1 more source

Anticancer Ruthenium Complexes with HDAC Isoform Selectivity

Molecules, 2020
The histone deacetylase (HDAC) enzymes have emerged as an important class of molecular targets in cancer therapy, with five inhibitors in clinical use. Recently, it has been shown that a lack of selectivity between the 11 Zn-dependent HDAC isoforms may ...
Jasmine M. Cross, Tim R. Blower, Alexander D. H. Kingdon, Robert Pal, David M. Picton, James W. Walton   +5 more
doaj   +1 more source

Solid-Phase Parallel Synthesis of Dual Histone Deacetylase-Cyclooxygenase Inhibitors

Molecules, 2023
Multi-target drugs (MTDs) are emerging alternatives to combination therapies. Since both histone deacetylases (HDACs) and cyclooxygenase-2 (COX-2) are known to be overexpressed in several cancer types, we herein report the design, synthesis, and ...
Luisa M. Bachmann, Maria Hanl, Felix Feller, Laura Sinatra, Andrea Schöler, Jens Pietzsch, Markus Laube, Finn K. Hansen   +7 more
doaj   +1 more source

Histone deacetylase inhibitors attenuated interleukin-1β-induced chondrogenesis inhibition in synovium-derived mesenchymal stem cells of the temporomandibular joint

Bone & Joint Research, 2022
Aims: In the repair of condylar cartilage injury, synovium-derived mesenchymal stem cells (SMSCs) migrate to an injured site and differentiate into cartilage.
Wen-ting Liao, Jia-dong Sun, Yun Wang, Yi-qing He, Kai Su, Yun-yang Lu, Guiqing Liao, Yang-peng Sun   +7 more
doaj   +1 more source

New histone deacetylase inhibitors as potential therapeutic tools for advanced prostate carcinoma [PDF]

, 2008
The anti-epileptic drug valproic acid is also under trial as an anti-cancer agent due to its histone deacetylase (HDAC) inhibitory properties. However, the effects of valproic acid (VPA) are limited and concentrations required for exerting anti ...
Atmaca, Akin, Batran, Salah-Eddin al-, Blaheta, Roman A., Hudak, Lukasz, Jonas, Dietger, Jüngel, Eva, Soldato, Piero Del, Sparatore, Anna, Wedel, Steffen Alexander   +8 more
core   +1 more source

Roles of histone deacetylases in epigenetic regulation: emerging paradigms from studies with inhibitors

Clinical Epigenetics, 2012
The zinc-dependent mammalian histone deacetylase (HDAC) family comprises 11 enzymes, which have specific and critical functions in development and tissue homeostasis.
Delcuve Geneviève P, Khan Dilshad H, Davie James R   +2 more
doaj   +1 more source

Synergistic interactions between HDAC and sirtuin inhibitors in human leukemia cells. [PDF]

PLoS ONE, 2011
Aberrant histone deacetylase (HDAC) activity is frequent in human leukemias. However, while classical, NAD(+)-independent HDACs are an established therapeutic target, the relevance of NAD(+)-dependent HDACs (sirtuins) in leukemia treatment remains ...
Michele Cea, Debora Soncini, Floriana Fruscione, Lizzia Raffaghello, Anna Garuti, Laura Emionite, Eva Moran, Mirko Magnone, Gabriele Zoppoli, Daniele Reverberi, Irene Caffa, Annalisa Salis, Antonia Cagnetta, Micaela Bergamaschi, Salvatore Casciaro, Ivana Pierri, Gianluca Damonte, Filippo Ansaldi, Marco Gobbi, Vito Pistoia, Alberto Ballestrero, Franco Patrone, Santina Bruzzone, Alessio Nencioni   +23 more
doaj   +1 more source

Inherited Retinal Degeneration: Towards the Development of a Combination Therapy Targeting Histone Deacetylase, Poly (ADP-Ribose) Polymerase, and Calpain

Biomolecules, 2023
Inherited retinal degeneration (IRD) represents a diverse group of gene mutation-induced blinding diseases. In IRD, the loss of photoreceptors is often connected to excessive activation of histone-deacetylase (HDAC), poly-ADP-ribose-polymerase (PARP ...
Yujie Dong, Jie Yan, Ming Yang, Wenrong Xu, Zhulin Hu, François Paquet-Durand, Kangwei Jiao   +6 more
doaj   +1 more source

Design, Synthesis and Biological Evaluation of Quinazolin-4-one Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.

Journal of Medicinal Chemistry, 2020
A series of quinazolin-4-one based hydroxamic acids was rationally designed and synthesized as novel dual PI3K/HDAC inhibitors by incorporating an HDAC pharmacophore into a PI3K inhibitor (Idelalisib) via an optimized linker.
Ashish Thakur, G. Tawa, M. Henderson, Carina Danchik, Suiyang Liu, P. Shah, Amy Q. Wang, Garrett Dunn, Md Kabir, E. C. Padilha, Xin Xu, A. Simeonov, S. Kharbanda, R. Stone, Gurmit S. Grewal   +14 more
semanticscholar   +1 more source

Quinolone-based HDAC inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2013
HDAC inhibitors emerged as promising drug candidates in combating wide variety of cancers. At present, two of the compounds SAHA and Romidepsin were approved by FDA for cutaneous T-cell lymphoma and many are in various clinical phases. A new quinolone cap structure was explored with hydroxamic acid as zinc-binding group (ZBG).
Gopalan, Balasubramanian, Narasimhan, Kilambi, Suresh, Rathinasamy, Praveen, Rajendran, Shridhar, Narayanan, Sridharan, Rajagopal   +5 more
openaire   +2 more sources