Results 1 to 10 of about 8,600 (184)

Non-Hydroxamate Zinc-Binding Groups as Warheads for Histone Deacetylases [PDF]

Molecules, 2021
Histone deacetylases (HDACs) remove acetyl groups from acetylated lysine residues and have a large variety of substrates and interaction partners. Therefore, it is not surprising that HDACs are involved in many diseases. Most inhibitors of zinc-dependent
Anton Frühauf, Franz-Josef Meyer-Almes
doaj   +5 more sources

Development of a Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-7/-13 Inhibitor [PDF]

Molecules, 2017
Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extracellular matrix proteins such as casein, gelatin, fibronectin and proteoglycan.
Thomas Fischer, Rainer Riedl
doaj   +5 more sources

TP0586532, a Novel Non-Hydroxamate LpxC Inhibitor: Potentiating Effect on In Vitro Activity of Meropenem against Carbapenem-Resistant Enterobacteriaceae [PDF]

Microbiology Spectrum, 2022
Carbapenem-resistant Enterobacteriaceae (CRE) are an urgent threat to public health requiring the development of novel therapies. TP0586532 is a novel non-hydroxamate LpxC inhibitor that inhibits the synthesis of lipopolysaccharides, which are components
Ippei Yoshida, Iichiro Takata, Kiyoko Fujita, Hajime Takashima, Hiroyuki Sugiyama   +4 more
doaj   +4 more sources

A Rational Approach for the Identification of Non-Hydroxamate HDAC6-Selective Inhibitors. [PDF]

Sci Rep, 2016
AbstractThe human histone deacetylase isoform 6 (HDAC6) has been demonstrated to play a major role in cell motility and aggresome formation, being interesting for the treatment of multiple tumour types and neurodegenerative conditions. Currently, most HDAC inhibitors in preclinical or clinical evaluations are non-selective inhibitors, characterised by ...
Goracci L, Deschamps N, Randazzo GM, Petit C, Dos Santos Passos C, Carrupt PA, Simões-Pires C, Nurisso A.   +7 more
europepmc   +5 more sources

Targeted HDAC8 inhibition with non-hydroxamate [1,2,4]triazolo[4,3-a] quinoline compounds [PDF]

Scientific Reports
Histone deacetylase 8 (HDAC8) is a key enzyme involved in regulating gene expression and tumor development, positioning it as an attractive target for neuroblastoma.
N. V. M. Rao Bandaru, Ashna Fathima, Suryansh Sengar, Markus Schweipert, Kosana Sai Chaitanya, Muzaffar-Ur-Rehman Mohammed, Suraj T. Gore, Trinath Jamma, Vivek Sharma, Chandrasekhar Abbineni, Franz-Josef Meyer-Almes, Kondapalli Venkata Gowri Chandra Sekhar   +11 more
doaj   +2 more sources

Next-Generation HDAC Inhibitors: Advancing Zinc-Binding Group Design for Enhanced Cancer Therapy [PDF]

Cells
Histone deacetylases (HDACs) are pivotal epigenetic regulators that control gene expression, cell proliferation, and differentiation, and their dysregulation is closely associated with the onset and progression of multiple cancers.
Mohammed Hawash
doaj   +2 more sources

Halting Tumor Progression via Novel Non-Hydroxamate Triazole-Based Mannich Bases MMP-2/9 Inhibitors; Design, Microwave-Assisted Synthesis, and Biological Evaluation. [PDF]

Int J Mol Sci, 2021
Matrix metalloproteinases (MMPs) are key signaling modulators in the tumor microenvironment. Among MMPs, MMP-2 and MMP-9 are receiving renewed interest as validated druggable targets for halting different tumor progression events. Over the last decades, a diverse range of MMP-2/9 inhibitors has been identified starting from the early hydroxamic acid ...
Albelwi FF, Teleb M, Abu-Serie MM, Moaty MNAA, Alsubaie MS, Zakaria MA, El Kilany Y, Aouad MR, Hagar M, Rezki N.   +9 more
europepmc   +2 more sources

Discovery and Characterization of Novel Non-Hydroxamate HDAC11 Inhibitors. [PDF]

Int J Mol Sci
Histone deacetylase 11 (HDAC11), the sole member of class IV HDACs, has gained prominence due to its unique enzymatic profile and pathological relevance in cancer, neurodegenerative, inflammatory diseases, and metabolic disorders. However, only a limited number of selective HDAC11 inhibitors have been identified, and many of these contain a potentially
Kopranovic A, Meyer-Almes FJ.
europepmc   +2 more sources

Biology of novel LpxC inhibitors for Neisseria gonorrhoeae informs strategy for therapeutic innovation [PDF]

Microbiology Spectrum
Historically, LpxC inhibitors, which target the UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase catalyzing the rate-limiting step in lipid A biosynthesis, have a hydroxamate zinc-chelating head group that targets the active site and can ...
Suzanne A. Otala, Constance M. John, Daniel C. Stein, Gary A. Jarvis   +3 more
doaj   +2 more sources

Total Synthesis of Talarolide A and atrop-Talarolide A: Hydroxamate H-Bond Bridge Stabilization of Cyclic Peptide Conformers Invokes Non-Canonical Atropisomerism [PDF]

Marine Drugs
The first total synthesis of the Australian marine tunicate fungus-derived cyclic peptide talarolide A (1) has confirmed the structure previously proposed on the basis of spectroscopic and chemical analyses and re-affirmed the importance of the unique ...
Waleed M. Hussein, Yuxuan Zhu, Angela A. Salim, Robert J. Capon   +3 more
doaj   +2 more sources