Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Peptide-Bismuth Tricycles: Maximizing Stability by Constraint.
Chemistry
January 2025
Australian National University, Research School of Chemistry, Sullivans Creek Road, ACT 2601, Canberra, AUSTRALIA.
Constrained peptides possess excellent properties for identifying lead compounds in drug discovery. While it has become increasingly straightforward to discover selective high-affinity peptide ligands, especially through genetically encoded libraries, their stability and bioavailability remain significant challenges. By integrating macrocyclization chemistry with bismuth binding, we generated series of linear, cyclic, bicyclic, and tricyclic peptides with identical sequences.
View Article and Find Full Text PDFA Mutant Complement Factor H (W1183R) Enhances Proteolytic Cleavage of von Willebrand Factor by ADAMTS13 Under Shear.
J Thromb Haemost
January 2025
Department of Pathology and Laboratory Medicine; Institute of Reproductive Medicine and Developmental Sciences, The University of Kansas Medical Center, Kansas City, KS 66160. Electronic address:
Background: A loss-of-functional mutation (W1183R) in human complement factor H (CFH) is associated with complement-associated hemolytic uremic syndrome; mice carrying a similar mutation (W1206R) in CFH also develop thrombotic microangiopathy but its plasma von Willebrand factor (VWF) multimer sizes were dramatically reduced. The mechanism underlying such a dramatic change in plasma VWF multimer distribution in these mice is not fully understood.
Objective And Methods: To determine the VWF and CFH interaction and how CFH proteins affect VWF multimer distribution, we employed recombinant protein expression, purification, and various biochemical and biophysical tools.
Identification of an exosite at the neutrophil elastase/alpha-1-antitrypsin interface.
FEBS J
January 2025
Physics, Department of Molecular and Translational Medicine, University of Brescia, Italy.
Neutrophil elastase (NE) is released by activated neutrophils during an inflammatory response and exerts proteolytic activity on elastin and other extracellular matrix components. This protease is rapidly inhibited by the plasma serine protease inhibitor alpha-1-antitrypsin (AAT), and the importance of this protective activity on lung tissue is highlighted by the development of early onset emphysema in individuals with AAT deficiency. As a serpin, AAT presents a surface-exposed reactive centre loop (RCL) whose sequence mirrors the target protease specificity.
View Article and Find Full Text PDFSynthesis and characterisation of DOTA-kisspeptin-10 as a potential gallium-68/lutetium-177 pan-tumour radiopharmaceutical.
J Neuroendocrinol
January 2025
Centre for Neuroendocrinology, University of Pretoria, Pretoria, South Africa.
Kisspeptin (KISS1) and its cognate receptor (KISS1R) are implicated in the progression of various cancers. A gallium-68 labelled kisspeptin-10 (KP10), the minimal biologically active structure, has potential as a pan-tumour radiopharmaceutical for the detection of cancers. Furthermore, a lutetium-177 labelled KP10 could find therapeutic application in treating oncological diseases.
View Article and Find Full Text PDFLiquid Chromatography Combined With Tandem Mass Spectrometry for the Pharmacokinetic and Metabolism Studies of PROTAC ARV-471 in Rats.
Biomed Chromatogr
February 2025
Department of Breast and Thyroid Surgery, The First Affiliated Hospital of University of Science and Technology of China, Anhui Provincial Hospital, Hefei, Anhui Province, China.
Article Synopsis
- PROTAC is a novel therapeutic approach gaining traction in pharmaceuticals, particularly for targeting proteins like estrogen receptors in breast cancer treatment.
- ARV-471 is an orally bioavailable PROTAC that effectively degrades estrogen receptors by promoting their degradation through the proteasome.
- A sensitive liquid chromatography method was developed to measure ARV-471 in rat plasma, demonstrating robust validation and revealing key metabolic pathways, including hydrolysis and glucuronidation, with four metabolites identified.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!