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The reuse of waste papers by conversion into valuable carbon materials has received considerable attention for diverse applications such as energy storage and water purification. However, traditional methods for converting waste papers into materials with suitable properties for specific applications are often complex and ineffective, involving consecutive carbonization and activation steps. Herein, we propose a simple one-step microwave (MW)-assisted synthesis for preparing waste paper-derived porous carbons (WPCs) for energy storage and water purification. Through a 30-min synthesis, WPCs with graphitic structure and high specific surface area were successfully produced. The fabricated WPCs exhibited outstanding charge storage capability with a maximum specific capacitance of 237.7 F g -1 . Additionally, the WPC demonstrates a high removal efficiency for various dyes, achieving a maximum removal efficiency of 95.0% for methylene blue. The developed one-step MW synthesis not only enables the production of porous carbon from waste paper, but also offers a viable approach to address solid waste management challenges while simultaneously yielding valuable materials., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

As the adverse effects of using plastics and perfluorinated alkyl substances become more apparent, there is a growing need for sustainable hydrophobic products. Cellulose and its derivatives are the most abundant and widely used polymers, and cellulose-based products have great potential in industries where plastics and other hydrophobic polymers are used, such as stain-resistant fabrics, food packaging, and oil-water separation applications. In this study, we extracted cellulose from water hyacinth (WH) biomass, known for its negative environmental impact, and converted it into hydrophobic cellulose. This addresses the issue of managing WH waste and creating an environmentally friendly hydrophobic material. Initially, aldehyde groups were introduced through oxidation with periodate, followed by direct octadecyl amine (ODA) grafting onto dialdehyde cellulose (DAC) via a Schiff base condensation. The resulting ODA modified cellulose (ODA-C) was dispersed in ethanol and used to coat various materials, including cotton fabric, cellulose filter paper, and packaging paper. The modified materials showed excellent hydrophobicity as measured by their water contact angles (WCAs), and the application of the coating was demonstrated for oil-water separation, stain-resistant hydrophobic fabric, and paper-based packaging materials. FTIR, XRD, and WCA analysis confirmed the successful modification of cellulose. A high separation efficiency of 99% was achieved for diesel/water separation using modified filter paper (MoFP), under gravity. On application of the coating, cotton fabric became hydrophobic and resisted staining from dye, and paper-based packaging materials became more robust by becoming water-resistant. Overall, the facile synthesis, low cost, high efficiency, and use of environmentally friendly sustainable materials make this a promising strategy for hydrophobically modifying surfaces for a wide range of applications while reducing the menace of water hyacinth., Competing Interests: Declaration of competing interest We declare that we have no known competing financial interests or personal relationships that could influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

P300 and CBP are two closely related histone acetyltransferases that are important transcriptional coactivators of many cellular processes. Inhibition of the transcriptional regulator p300/CBP is a promising therapeutic approach in oncology. However, there are no reported single selective p300 or CBP inhibitors to date. In this study, we designed and optimized a series of lysine acetyltransferase p300 selective inhibitors bearing a nucleoside scaffold. Most compounds showed excellent inhibitory activity against p300 with IC 50 ranging from 0.18 to 9.90 μM, except for J16, J29, J40, and J48. None of the compounds showed inhibitory activity against CBP (inhibition rate < 50 % at 10 µM). Then the cytotoxicity of the compounds against a series of cancer cells were evaluated. Compounds J31 and J32 showed excellent proliferation inhibitory activity on cancer cells T47D and H520 with desirable selectivity profile of p300 over CBP. These compounds could be promising lead compounds for the development of novel epigenetic inhibitors as antitumor agents., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

FR901464 is a natural product that exhibits antiproliferative activity at single-digit nanomolar concentrations in cancer cells. Its tetrahydropyran-spiroepoxide covalently binds the spliceosome. Through our medicinal chemistry campaign, we serendipitously discovered that a bromoetherification formed a tetrahydrofuran. The tetrahydrofuran analog was three orders of magnitude less potent than the corresponding tetrahydropyran analogs. This study shows the significance of the tetrahydropyran ring that presents the epoxide toward the spliceosome., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: John C. Schmitz reports financial support was provided by UPMC Hillman Cancer Center NCI Cancer Center Support Grant Developmental Funds. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

Leukocyte antigen-related (LAR) phosphatase is a receptor-type protein tyrosine phosphatase involved in cellular signaling and associated with human disease including cancer and metabolic disorders. Selective inhibition of LAR phosphatase activity by well characterized and well validated small molecules would provide key insights into the roles of LAR phosphatase in health and disease, but identifying selective inhibitors of LAR phosphatase activity has been challenging. Recently, we described potent and selective inhibition of LAR phosphatase activity by the fungal natural product illudalic acid. Here we provide a detailed biochemical characterization of the adduct formed between LAR phosphatase and illudalic acid. A mass spectrometric analysis indicates that two cysteine residues are covalently labeled by illudalic acid and a related analog. Mutational analysis supports the hypothesis that inhibition of LAR phosphatase activity is due primarily to the adduct with the catalytic cysteine residue. A computational study suggests potential interactions between the illudalic acid moiety and the enzyme active site. Taken together, these data offer novel insights into the mechanism of inhibition of LAR phosphatase activity by illudalic acid., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

Copper plays a crucial role in maintaining biological redox balance in living organisms, with elevated levels observed in cancer cells. Short interfering RNAs (siRNAs) are effective in gene silencing and find applications as both research tools and therapeutic agents. A method to regulate RNA interference using copper is especially advantageous for cancer-specific therapy. We present a chemical approach of selective siRNA activation triggered by intracellular copper ions. We designed and synthesized nucleotides containing copper-responsive moieties, which were incorporated into siRNAs. These copper-responsive siRNAs effectively silenced the target cyclin B1 mRNA in living cells. This pioneering study introduces a novel method for conditionally controlling gene silencing using biologically relevant metal ions in human cells, thereby expanding the repertoire of chemical knockdown tools., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Akimitsu Okamoto reports financial support was provided by Japan Society for the Promotion of Science. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Osteoporosis is a progressive systemic skeletal disease that decreases bone density and bone quality, making them fragile and easy to break. In spite of effective anti-osteoporosis potency, teriparatide, the first anabolic medications approved for the treatment of osteoporosis, was proven to exhibit various side effects. And the relevant structure-activity relationship (SAR) of teriparatide was in need. In this work, we performed a systematical alanine scanning against teriparatide and synthesized 34 teriparatide derivatives. Their biological activities were evaluated and the importance of each residue for anti-osteoporosis activity was also revealed. A remarkable decrease in activity was observed for alanine replacement of the residue Gly 12 , His 14 , Ser 17 , Arg 20 and Leu 24 , showcasing the important role of these residues in teriparatide on anti-osteoporosis activity. On contrary, when Gly 13 and Gln 30 were mutated to Ala, the peptide derivatives exhibited the significantly increased activities, demonstrating that these two residues could be readily replaced. Our research expanded the peptide library of teriparatide analogues and presented a potential opportunity for designing the more powerful anti-osteoporosis peptide agents., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

Aptamers have shown significant potential in treating diverse diseases. However, challenges such as stability and drug delivery limited their clinical application. In this paper, the development of AS1411 prodrug-type aptamers for tumor treatment was introduced. A Short oligonucleotide was introduced at the end of the AS1411 sequence with a disulfide bond as responsive switch. The results indicated that the aptamer prodrugs not only enhanced the stability of the aptamer against nuclease activity but also facilitated binding to serum albumin. Furthermore, in the reducing microenvironment of tumor cells, disulfide bonds triggered drug release, resulting in superior therapeutic effects in vitro and in vivo compared to original drugs. This paper proposes a novel approach for optimizing the structure of nucleic acid drugs, that promises to protect other oligonucleotides or secondary structures, thus opening up new possibilities for nucleic acid drug design., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

β-galactosidase (β-gal) has high activity in various malignancies, which is suitable for targeted positron emission tomography (PET) imaging. Meanwhile, β-gal can successfully guide the formation of nanofibers, which enhances the intensity of imaging and extends the imaging time. Herein, we designed a β-galactosidase-guided self-assembled PET imaging probe [ 68 Ga]Nap-NOTA-1Gal. We envisage that β-gal could recognize and cleave the target site, bringing about self-assembling to form nanofibers, thereby enhancing the PET imaging effect. The targeting specificity of [ 68 Ga]Nap-NOTA-1Gal for detecting β-gal activity was examined using the control probe [ 68 Ga]Nap-NOTA-1. Micro-PET imaging showed that tumor regions of [ 68 Ga]Nap-NOTA-1Gal were visible after injection. And the tumor uptake of [ 68 Ga]Nap-NOTA-1Gal was higher than [ 68 Ga]Nap-NOTA-1 at all-time points. Our results demonstrated that the [ 68 Ga]Nap-NOTA-1Gal can be used for the purpose of a new promising PET probe for helping diagnose cancer with high levels of β-gal activity., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

Antascomicin B is a natural product that similarly to the macrolides FK506 and Rapamycin binds to the FK506-binding protein 12 (FKBP12). FK506 and Rapamycin act as molecular glues by inducing ternary complexes between FKBPs and additional target proteins. Whether Antascomicin B can induce ternary complexes is unknown. Here we show that Antascomicin B binds tightly to larger human FKBP homologs. The cocrystal structure of FKBP51 in complex with Antascomicin B revealed that large parts of Antascomicin B are solvent-exposed and available to engage additional proteins. Cellular studies demonstrated that Antascomicin B enhances the interaction between human FKBP51 and human Akt. Our studies show that molecules with molecular glue-like properties are more prominent in nature than previously thought. We predict the existence of additional 'orphan' molecular glues that evolved to induce ternary protein complexes but where the relevant ternary complex partners are unknown., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Felix Hausch reports financial support was provided by Technical University of Darmstadt. Felix Hausch reports a relationship with Federal Ministry of Education and Research Berlin Office that includes: funding grants. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Crown Copyright © 2024. Published by Elsevier Ltd. All rights reserved.)