Slow-Binding and Covalent HDAC Inhibition: A New Paradigm?

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Colorectal cancer (CRC) is among the three most commonly diagnosed cancers and one of the major causes of cancer-related morbidity and mortality. Despite the discovery of several predictive biomarkers, the 5-year survival rate for metastatic CRC is 15%. A ...

Cancer drug resistance remains a critical challenge in oncology, demanding rapid and reliable diagnostic tools to assess tumor cell susceptibility to treatment. This study presents a nanomotion-based drug susceptibility testing (DST) approach, integrating ...

Cysteine cathepsins are a family of proteases that are relevant therapeutic targets for the treatment of different cancers and other diseases. However, no clinically approved drugs for these proteins exist, as their systemic inhibition can induce deleterio ...

Classical Zn2+-dependent deac(et)ylases play fundamental regulatory roles in life and are well characterized in eukaryotes regarding their structures, substrates and physiological roles. In bacteria, however, classical deacylases are less well understood. ...

ABCG2 is an ATP-binding cassette transporter that exports a wide range of xenobiotic compounds and has been recognized as a contributing factor for multidrug resistance in cancer cells. Substrate and inhibitor interactions with ABCG2 have been extensively ...

Retinoblastoma is the most common pediatric eye cancer. It is currently treated with a limited number of drugs, adapted from other pediatric cancer treatments. Drug toxicity and relapse of the disease warrant new therapeutic strategies for these young pati ...

Etoposide (ETO) and methotrexate (MTX) are widely used chemotherapy drugs in cancer treatment, targeting specific cellular processes crucial for DNA replication and cell division. Despite their efficacy, both drugs have significant adverse toxic effects du ...

For several years, drugs with reactive electrophilic appendages have been developed. These units typically confer prolonged residence time of the drugs on their protein targets, and may assist targeting shallow binding sites and/or improving the drug-prote ...

Although genomic DNA is the primary target of anticancer platinum-based drugs, interactions with proteins also play a significant role in their overall activity. In this study, competitive binding of cisplatin with an oligonucleotide and two peptides corre ...

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...

Emerging evidence suggests that hierarchical status provide vulnerability to develop stress-induced depression. Energy metabolic changes in the nucleus accumbens (NAc) were recently related to hierarchical status and vulnerability to develop depression-lik ...

Major depression is a highly complex disabling psychiatric disorder affecting millions of people worldwide. Despite the availability of several classes of antidepressants, a substantial percentage of patients are unresponsive to these medications. A better ...

The design of multitarget-directed ligands is a promising strategy for discovering innovative drugs. Here, we report a mechanistic study that clarifies key aspects of the dual inhibition of the fatty acid amide hydrolase (FAAH) and the cyclooxygenase (COX) ...

Two bifunctional ruthenium(II)-p-cymene complexes with perfluorinated side chains, attached via pyridine ligands, have been evaluated in a series of in vitro and in vivo assays. Their effects on human endothelial (ECRF24 and HUVEC) cells, noncancerous huma ...

The current understanding of epigenetic signaling assigns a central role to post-translational modifications that occur in the histone tails. In this context, it has been proposed that methylation of K9 and phosphorylation of S10 in the tail of histone H3 ...

Combinatorial libraries of structurally diverse peptide macrocycles offer a rich source for the development of high-affinity ligands to targets of interest. In this work we have developed linkers for the generation of genetically encoded bicyclic peptides ...

Slow-Binding and Covalent HDAC Inhibition: A New Paradigm?

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Abstract 4588: Cell states and resistance in colorectal cancer: What can we learn from patient-derived organoids?

Nanomotion-Based Drug Sensitivity Prediction in Ovarian and Colon Cancer Cell Lines Using Machine Learning

Antibody-peptide conjugates deliver covalent inhibitors blocking oncogenic cathepsins

Distribution and diversity of classical deacylases in bacteria

Structural Basis of the Allosteric Inhibition of Human ABCG2 by Nanobodies

Translational screening platform to evaluate chemotherapy in combination with focal therapy for retinoblastoma

Simultaneous and Selective Detection of Etoposide and Methotrexate With Single Electrochemical Sensors for Therapeutic Drug Monitoring

Can Precision Electrophile Signaling Make a Meaningful and Lasting Impression in Drug Design?

Simultaneous mass spectrometry analysis of cisplatin with oligonucleotide-peptide mixtures: implications for the mechanism of action

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Metabolic signature in nucleus accumbens for anti-depressant-like effects of acetyl-L-carnitine

The HDAC inhibitor SAHA improves depressive-like behavior of CRTC1-deficient mice: Possible relevance for treatment-resistant depression

The Molecular Basis for Dual Fatty Acid Amide Hydrolase (FAAH)/Cyclooxygenase (COX) Inhibition

Antiangiogenic and Anticancer Properties of Bifunctional Ruthenium(II)-p-Cymene Complexes: Influence of Pendant Perfluorous Chains

Structural Role of RKS Motifs in Chromatin Interactions: A Molecular Dynamics Study of HP1 Bound to a Variably Modified Histone Tail

Structurally Diverse Cyclisation Linkers Impose Different Backbone Conformations in Bicyclic Peptides