Thomas H. Schrader

Modulation of Epigenetic Control by Advanced Molecular Tweezers

My‐Hue‐Le, Bianca E. Kamba, Anja Matena, Christine Beuck et autres

This work addresses the question if supramolecular systems can be tailored to interfere with posttranslational modifications (PTM) and epigenetics. As a prominent example, the efficient epigenetic control operative in nucleosome-DNA interactions was selected. Conceptually, transcription activation by specific acetylation of strategic lysine …

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Molecular tweezer–peptide conjugates disrupt the protein–protein interaction between survivin and histone H3 essential in mitosis

Catherine Gsell, Philipp Rebmann, Karina Opara, Christine Beuck et autres

Peptide-modified supramolecular tweezers, a promising new class of chemical tools, were designed and employed to inhibit the interaction of the BIR domain of human survivin, a member of the chromosomal passenger complex (CPC), with the phosphorylated histone H3 N-terminal peptide. Fluorescence polarization …

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Allosteric Modulation of Pathological Ataxin‐3 Aggregation: A Path to Spinocerebellar Ataxia Type‐3 Therapies (Adv. Sci. 11/2026)

Alexandra Silva, Sara Duarte‐Silva, Pedro Miguel Martins, Beatriz Rodrigues et autres

Advanced Molecular Tweezers Effectively Target Membranes Lacking Choline Headgroups for Broad-Spectrum Antiviral Efficacy

Tatjana Weil, Jan Lawrenz, Estelle Taghuo Kaptouom, Joel Mieres-Perez et autres

Broad-spectrum antivirals are urgently required to counter present and emerging viral threats. It has previously been shown that the parental molecular tweezers CLR01 and CLR05 disrupt viral envelopes by complexing choline headgroups and that ester-functionalized "advanced" tweezers display markedly enhanced antiviral potency. …

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Allosteric Modulation of Pathological Ataxin‐3 Aggregation: A Path to Spinocerebellar Ataxia Type‐3 Therapies

Alexandra Silva, Sara Duarte‐Silva, Pedro Miguel Martins, Beatriz Rocha Ilidio Rodrigues et autres

Spinocerebellar ataxia type 3 (SCA3) is a rare neurodegenerative disorder caused by the expansion of a polyglutamine (polyQ) repeat in ataxin-3 (Atx3) for which no disease-modifying therapies are available. The presence of protein inclusions enriched in polyQ-expanded Atx3 in neurons suggests that …

fr, pt, de, gb, us (code pays fourni par la source)

Strategic implementation of HPV vaccination to eliminate cervical cancer in Georgia

Irakli Khuntsaria, Konstantine Gachechiladze, Elene Liparta, Tamar Kobulashvili et autres

Objectives: Human Papillomavirus (HPV) is a prevalent sexually transmitted infection and a leading cause of cervical cancer. In Georgia, cervical cancer ranks as the fifth most common cancer among women, with approximately 330 new cases and 200 deaths reported annually. Despite the …

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Monitoring Receptor Clustering by Aggregation‐Induced Emission

Robert Bekus, Kevin Rudolph, Steffen Riebe, Jens Voskuhl et autres

This study introduces a simple signal transduction system that mimics the receptor tyrosine kinase mechanism by employing amphiphilic receptors embedded in lipid bilayers. The designed receptors carry bisphosphonate head groups and feature aggregation-induced emission enhancement (AIEE) properties. Upon addition of polyammonium messengers, …

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Highly Preorganized Calixarene Tweezers for Protein Recognition

Katrin Hommel, Sebastian Theisen, Mike Blueggel, Felix C. Niemeyer et autres

Calixarene scaffolds offer structural robustness and tunable geometry for designing selective supramolecular inhibitors. Here, we developed a focused library of preorganized multivalent calix[4]arene tweezers targeting the cancer-related protease Taspase 1. Seven cone-conformation derivatives were synthesized, varying in linker rigidity, functionalization, and multivalency. …

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Molecular Tweezers Block the Functional Pore of a Protein Machine

Abbna Kirupakaran, Johannes van den Boom, Mike Blueggel, Christine Beuck et autres

High Resolution Image Download MS PowerPoint Slide We present symmetric multivalent tweezers as the first class of supramolecular elements designed to cover and functionally block a protein pore. As a model, we chose the enzyme p97, a hexameric AAA-ATPase that unfolds or …

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Allosteric Modulation of Pathological Ataxin-3 Aggregation: A Path to Spinocerebellar Ataxia Type-3 Therapies

Alexandra Silva, Sara Duarte‐Silva, Pedro Miguel Martins, Beatriz Rodrigues et autres

Spinocerebellar ataxia type 3 (SCA3) is a rare inherited neurodegenerative disease caused by the expansion of a polyglutamine repeat in the protease ataxin-3 (Atx3). Despite extensive knowledge of the downstream pathophysiology, no disease-modifying therapies are currently available to halt disease progression. The …

fr, pt, de, gb, us (code pays fourni par la source)

Photoresponsive molecular tweezers modulate Taspase 1 activity

Antonio L. Figueroa Bietti, Alisa-Maite A. Kauth, Katrin Hommel, Mike Blueggel et autres

-isomers of larger tweezers exhibited powerful enzyme inhibition, likely due to their ability to bridge lysines flanking the active site. This photoswitchable tweezer system provides a versatile tool for light-controlled modulation of protein function, offering new opportunities for selectively targeting lysine-rich proteins …

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Anti-amyloid treatment is broadly effective in neuronopathic mucopolysaccharidoses and synergizes with gene therapy in MPS-IIIA

Giaccio Marianna, Antonio Monaco, Galiano Laura, Parente Andrea et autres

Mucopolysaccharidoses (MPSs) are childhood diseases caused by inherited deficiencies in glycosaminoglycan degradation. Most MPSs involve neurodegeneration, which to date is untreatable. Currently, most therapeutic strategies aim at correcting the primary genetic defect. Among these strategies, gene therapy has shown great potential, although …

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