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http://dx.doi.org/10.1038/s41421-024-00711-x | DOI Listing |
Bioorg Chem
January 2025
Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education and Research (NIPER), Kolkata, West Bengal 700054, India. Electronic address:
Recent years have witnessed notable breakthroughs in the field of biotherapeutics. Proteolysis Targeting Chimeras (PROTACs) are novel molecules which used to degrade particular proteins despite the blockage by small drug molecules, which leads to a predicted therapeutic activity. This is a unique finding, especially at the cellular level targets degradations.
View Article and Find Full Text PDFCancers (Basel)
October 2024
Division of Hematology, Department of Medicine, University of Miami and Sylvester Comprehensive Cancer Center, Miami, FL 33136, USA.
B-cell lymphoid malignancies are a heterogeneous group of hematologic cancers, where Bruton's tyrosine kinase (BTK) inhibitors have received FDA approval for several subtypes. The first-in-class covalent BTK inhibitor, Ibrutinib, binds to the C481 amino acid residue to block the BTK enzyme and prevent the downstream signaling. Resistance to covalent BTK inhibitors (BTKi) can occur through mutations at the BTK binding site (C481S) but also other BTK sites and the phospholipase C gamma 2 (PLCγ2) resulting in downstream signaling.
View Article and Find Full Text PDFACS Omega
September 2024
AnHorn Medicines Co., Ltd., Taipei 115202, Taiwan.
The rational design of novel drug candidates presents a formidable challenge in modern drug discovery. Proteolysis-targeting chimeras (PROTACs) drug design is particularly demanding due to their limited crystal structure availability and design of a viable small molecule to bridge the protein of interest (POI) and ubiquitin-protein ligase (E3). An integrated approach that combines superimposition techniques and deep neural networks is demonstrated in this study to leverage the power of deep learning and structural biology to generate structurally diverse molecules with enhanced binding affinities.
View Article and Find Full Text PDFCells
July 2024
Institute of Molecular Medicine and Cell Research, IMMZ, Faculty of Medicine, University of Freiburg, 79104 Freiburg, Germany.
Signaling proteins in eukaryotes usually comprise a catalytic domain coupled to one or several interaction domains, such as SH2 and SH3 domains. An additional class of proteins critically involved in cellular communication are adapter or scaffold proteins, which fulfill their purely non-enzymatic functions by organizing protein-protein interactions. Intriguingly, certain signaling enzymes, e.
View Article and Find Full Text PDFCell Discov
August 2024
State Key Laboratory of Membrane Biology, School of Life Sciences, Tsinghua-Peking Center for Life Sciences, Institute for Immunology, Ministry of Education Key Laboratory of Protein Sciences, Beijing Key Lab for Immunological Research on Chronic Diseases, Beijing Tsinghua Changgeng Hospital, Tsinghua University, Beijing, China.
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