Author

G. Keserű

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Open access Sep 2026

Fragment‐Based Screening of Heterocyclic Electrophiles Identified Acrylamide Bioisoteres for Covalent KRasG12C Inhibitors

Covalent fragment approaches gained increasing attention in medicinal chemistry. Our covalent heterocyclic fragment library (Covalent MiniFrags) consisting of five and six membered heterocycles was screened against the oncogenic target KRasG12C. First, we detected the labeling of cysteine residues by Ellman's free thio...

Nikolett Péczka, Aaron B. Keeley, Péter Ábrányi-Balogh et al. · Archiv der Pharmazie · 0 citations

Review Open access Aug 2026

Disulfide rebridging platforms for site-specific ADC conjugation

Antibody–drug conjugates (ADCs) have emerged as a transformative class of targeted therapeutics, combining the exquisite specificity of monoclonal antibodies with the potency of small-molecule cytotoxic payloads. While numerous strategies exist to generate ADCs, site-specific conjugation methods have gained prominence...

L. Petri, Írisz K. Kovács, Blanka J Kiss et al. · RSC Chemical Biology · 0 citations

Open access Aug 2026

The structure of the dopamine D3 receptor bound to cariprazine reveals principles for partial agonists with designed pharmacology

The third-generation antipsychotic cariprazine is a low-efficacy partial agonist of the dopamine D3 receptor (D3R). Here, we report the cryo–electron microscopy structure of cariprazine bound to D3R, establishing a framework for understanding ligand recognition in this receptor. We further determine structures of D3R i...

Eliane Hadas Yardeni, Dóra Judit Kiss, Julie Sanchez et al. · Science Advances · 0 citations