In situ proteolysis is the method of proactively adding tiny amounts of nonspecific proteases to aid in the crystallization of proteins and protein macromolecular complexes. The simplicity of the procedure and high recovery rate make it a method of first choice for recalcitrant targets. An improved and updated in situ proteolysis protocol used in high-throughput structural biology platforms is described.
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http://dx.doi.org/10.1007/978-1-4939-0354-2_14 | DOI Listing |
Angew Chem Int Ed Engl
December 2024
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Nanjing, Jiangsu, 211198, China.
Proteolysis targeting chimeras (PROTACs) hold immense promise for targeted protein degradation; however, challenges such as off-target effects, poor drug-likeness properties, and the "hook effect" remain. This study introduces Nano-Click-formed PROTACs (Nano-CLIPTACs) for precise tumor protein degradation in vivo. Traditional PROTACs with high molecular weight were first divided into two smaller druglike precursors capable of self-assembling to form functional PROTACs through a bioorthogonal reaction.
View Article and Find Full Text PDFCancers (Basel)
December 2024
Laboratory of Experimental Pathology, Gonçalo Moniz Institute, Oswaldo Cruz Foundation, 121 Rua Waldemar Falcão, Salvador 40296-710, BA, Brazil.
The present study investigates VKINE, a bioactive proteolytic fragment of the proteoglycan VCAN, as a novel and significant element in the tumor extracellular matrix (ECM). Although VKINE has been recognized for its immunomodulatory potential in certain tumor types, its impact on ECM degradation and prognostic implications remains poorly understood. : This study aimed to evaluate VCAN proteolysis and its association with ADAMTS enzymes involved in extracellular matrix remodeling in spontaneous canine mammary gland cancer.
View Article and Find Full Text PDFPeerJ
December 2024
Sichuan Key Laboratory of Conservation Biology for Endangered Wildlife, Chengdu, Sichuan, China.
Background: The reproductive ability of male giant pandas has been a major complicating factor in the conservation of the species. While it is well known that the testis produces sperm and secretes androgens, a process that requires precise regulation of various proteins, at present, there has been no systematic study on the composition of proteins in the testis of the giant pandas. Therefore, this study aims to apply proteomics to explore the regulation of proteins in the testes of giant pandas.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
School of Material Science and Food Engineering, University of Electronic Science and Technology of China, Zhongshan Institute, 1 Xueyuan Road, Zhongshan 528402, Guangdong Province, People's Republic of China.
Transl Neurodegener
November 2024
Department of Pharmacology and Chemical Biology, Shanghai Jiao Tong University School of Medicine, Shanghai, 200025, China.
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