Results 11 to 20 of about 8,600 (184)

Development of the first non-hydroxamate selective HDAC6 degraders [PDF]

Chemical Communications, 2022
The targeted degradation of histone deacetylase 6 (HDAC6) by heterobifunctional degraders constitutes a promising approach to treat HDAC6-driven diseases. Previous HDAC6 selective degraders utilised a hydroxamic acid as a zinc-binding group (ZBG) which features mutagenic and genotoxic potential.
Tim Keuler, Beate König, Nico Bückreiß, Fabian B. Kraft, Philipp König, Linda Schäker-Hübner, Christian Steinebach, Gerd Bendas, Michael Gütschow, Finn K. Hansen   +9 more
core   +5 more sources

Developing novel non-hydroxamate histone deacetylaseinhibitors: the chelidamic warhead [PDF]

MedChemComm, 2012
The dimethyl 4-hydroxypyridine-2,6-dicarboxylate is a valuable scaffold for HDAC inhibitor design as a replacement of the well-known hydroxamate function.
Valente, Sergio, Conte, Mariarosaria, Tardugno, Maria, Nebbioso, Angela, Tinari, Gabriella, Altucci, Lucia, Mai, Antonello   +6 more
openaire   +5 more sources

Design, synthesis, and biological evaluation of substituted benzyl-triazolopyridine derivatives as non-hydroxamate based HDAC8 inhibitors

European Journal of Medicinal Chemistry Reports
Traditional Histone deacetylase 8 (HDAC8) inhibitors primarily rely on hydroxamate-based scaffolds. However, there is a growing interest in developing non-hydroxamate inhibitors to overcome potential limitations with hydroxamate-based inhibitors. In this
N.V.M. Rao Bandaru, Ashna Fathima, Vandana Joshi, Markus Schweipert, Obanna Pathur, Kosana Sai Chaitanya, Trinath Jamma, Vivek Sharma, Chandrasekhar Abbineni, Franz-Josef Meyer-Almes, Kondapalli Venkata Gowri Chandra Sekhar   +10 more
doaj   +2 more sources

Integrative computational approaches identify haptoglobin inhibitors to modulate erythrocyte sedimentation rate in trauma-linked inflammatory and haematological malignancies [PDF]

Frontiers in Chemistry
Elevated levels of haptoglobin are commonly observed in conditions characterised by an increased erythrocyte sedimentation rate which are acute-phase reactants.
Abdulaziz H. Al Khzem, Shaban Ahmad
doaj   +2 more sources

Strain-specific activation of aspergillic acid biosynthesis in Aspergillus oryzae NRRL 3483 [PDF]

Scientific Reports
Aspergillic acid, a hydroxamate-containing pyrazinone derived from leucine and isoleucine, is a hallmark metabolite of Aspergillus flavus, which also produces the potent carcinogen aflatoxin. Its biosynthesis is governed by the recently characterized asa
Dasol Choi, Xingrui Fan, Hee-Soo Park, Jae-Hyuk Yu   +3 more
doaj   +2 more sources

Design, Synthesis, Bioactivity Evaluation, Crystal Structures, and In Silico Studies of New α-Amino Amide Derivatives as Potential Histone Deacetylase 6 Inhibitors

Molecules, 2022
Hydroxamate, as a zinc-binding group (ZBG), prevails in the design of histone deacetylase 6(HDAC6) inhibitors due to its remarkable zinc-chelating capability.
Yangrong Xu, Hangjun Tang, Yijie Xu, Jialin Guo, Xu Zhao, Qingguo Meng, Junhai Xiao   +6 more
doaj   +1 more source

Non-Hydroxamate Histone Deacetylase Inhibitors [PDF]

Current Medicinal Chemistry, 2005
A number of histone deacetylase (HDAC) inhibitors have been developed as anticancer agents and most of them are hydroxamic acid derivatives, typified by suberoylanilide hydroxamic acid (SAHA), Trichostatin A (TSA) and NVP-LAQ824. However, hydroxamic acids have been associated with poor pharmacokinetics and severe toxicity. In addition, although isozyme-
Takayoshi, Suzuki, Naoki, Miyata
openaire   +2 more sources

Selection and characterization of siderophores of pathogenic Escherichia coli intestinal and extraintestinal isolates

Open Agriculture, 2021
Microorganisms adopt a unique mechanism for sequestration and transport of bound iron by producing iron-chelating molecules called siderophores. Siderophores play an important role in colonization of microbes in iron-deficient sites of the host, hence ...
Kumar Gulshan, Kumar Yashwant, Kumar Gaurav, Tahlan Ajay Kumar   +3 more
doaj   +1 more source

Matrix Metalloproteinase Inhibition in Melanoma. [PDF]

Exp Dermatol
ABSTRACT Matrix metalloproteinases (MMPs) are involved in the degradation of the extracellular matrix (ECM) and are found to participate in all stages of tumour progression including modifying signalling pathways, regulating cytokines and promoting tumour growth, particularly by inducing angiogenesis and facilitating cancer spread.
Zhang E, Thakur V, Bedogni B.
europepmc   +2 more sources

Bacterial Zinc Metalloenzyme Inhibitors: Recent Advances and Future Perspectives [PDF]

, 2023
Human deaths caused by Gram-negative bacteria keep rising due to the multidrug resistance (MDR) phenomenon. Therefore, it is a priority to develop novel antibiotics with different mechanisms of action.
Cuffaro, Doretta, Di Leo, Riccardo, Nuti, Elisa, Rossello, Armando   +3 more
core   +1 more source