Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Histone deacetylase (HDAC) inhibitors are approved as cancer chemotherapy and studied for the treatment of various diseases. However, there is a lack of isozyme-selective compounds to determine the biological role of each of the 11 HDACs, and to develop drugs applicable to a wider range of disorders. Here, we describe the synthesis of hydroxamic acid and trifluoromethyl ketone-containing building blocks and their use to synthesize libraries of HDAC-binding peptides. Modified peptides are synthesized via the SPOT method on cellulose discs that allow deprotection and solubilization to obtain printable DMSO stocks, which afford hundreds of library copies on assay-ready slides. Thus, multiple screening rounds can be performed on a single library. This method facilitates the screening of peptides as potential HDAC inhibitors with diverse selectivity and has already provided compounds active in cells.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/978-1-0716-4578-9_11 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Self-Assembled Polypseudorotaxanes Crosslinked by Dynamic Disulfide Bonds as Modular Functionalization for Thiophilic Metal Nanoparticles.
Angew Chem Int Ed Engl
September 2025
Institute of Pharmaceutical Science, King's College London, Franklin Wilkins Building, Stamford Street, London, SE1 9NH, UK.
As supramolecular assemblies, polypseudorotaxanes (PPR) exhibit inherent advantages in modular adaptability and structural programmability, with the potential to build tuneable platforms integrating various functionalities. Here we report the "one-pot" preparation of a self-assembled thiol-rich PPR (SPPR), where thiolated-α-cyclodextrins (SHαCD) spontaneously thread onto polymers, and are then crosslinked into a three-dimensional network by the thermally-triggered oxidation of thiols into disulfide bonds. The dynamic thiol groups along the SPPR provide remarkable modularity for the functionalization of thiophilic metal nanoparticles (NPs), exemplified by two application vectors.
View Article and Find Full Text PDFOptimising parent selection in plant breeding: comparing metaheuristic algorithms for genotype building.
Theor Appl Genet
September 2025
Queensland Alliance for Agriculture and Food Innovation, University of Queensland, Brisbane, Australia.
Stacking desirable haplotypes across the genome to develop superior genotypes has been implemented in several crop species. A major challenge in Optimal Haplotype Selection is identifying a set of parents that collectively contain all desirable haplotypes, a complex combinatorial problem with countless possibilities. In this study, we evaluated the performance of metaheuristic search algorithms (MSAs)-genetic algorithm (GA), differential evolution (DE), particle swarm optimisation (PSO), and simulated annealing (SA) for optimising parent selection under two genotype building (GB) objectives: Optimal Haplotype Selection (OHS) and Optimal Population Value (OPV).
View Article and Find Full Text PDFBranched DNA for disease diagnosis and therapy.
Adv Drug Deliv Rev
September 2025
State Key Laboratory of Systems Medicine for Cancer, Shanghai Cancer Institute, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200032, China; Shanghai Key Laboratory of Cancer System Regulation and Clinical Translation, Jiading District Central Hospital, Renji Hospital J
DNA exhibits remarkable versatility, which is attributed to its inherent molecular recognition capabilities, programmable sequences, and excellent biocompatibility. Among its various topological forms, branched DNA (bDNA), including Y-shaped DNA (Y-DNA), X-shaped DNA (X-DNA), etc., stands out as a fundamental building block for fabricating functional DNA-based materials and has demonstrated great promise across diverse applications in recent years.
View Article and Find Full Text PDFC2-Benzylic C(sp)-H Alkylation of Indoles Enabled by Photoinduced, EDA-Complex-Mediated Radical-Radical Cross-Coupling.
Org Lett
September 2025
College of Chemistry and Chemical Engineering, Central South University, Changsha 410083, P. R. China.
2-Alkylindoles are privileged motifs that serve as versatile intermediates and building blocks in synthetic and medicinal chemistry. Herein, we report a photoinduced, EDA-complex-enabled C2-benzylic C(sp)-H alkylation of indoles with bromides through radical cross-coupling. This developed protocol provides facile access to 2-alkylindoles from structurally varied 2-methylindoles and bromides under mild reaction conditions with simple operation.
View Article and Find Full Text PDFAdvances in the Catalytic Asymmetric Synthesis of Chiral α-Aryl Ketones.
Chem Rec
September 2025
Department of Chemistry, St. Thomas College Palai, Arunapuram P.O., Kottayam, Kerala, 686574, India.
An α-aryl-substituted enantioenriched ketone is a valuable building block for the production of both natural and medicinal compounds. Research into their asymmetric synthesis can be challenging yet rewarding because of the need to control regio-, chemo-, and enantioselectivity carefully. A wide range of catalytic strategies has been developed during the past three decades to gain access to these favored motifs.
View Article and Find Full Text PDF