Purified recombinant prohormone convertase 1 and 2 (PC1 and PC2) cleave a peptide containing cholecystokinin (CCK) 8 Gly Arg Arg and the carboxyl-terminal peptide liberating CCK 8 Gly Arg Arg. PC1 and PC2 also cleave purified pro CCK, liberating the amino terminal pro-peptide while no carboxyl-terminal cleavage was detected. Under the conditions of the in vitro cleavage assay, it appears that the carboxyl-terminal cleavage site of pro CCK is not accessible to the enzymes while this site is readily cleaved in a synthetic peptide. Additional cellular proteins that unfold the prohormone may be required to expose the carboxyl-terminal site for cleavage.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.peptides.2005.05.006 | DOI Listing |
BMC Pharmacol Toxicol
August 2024
Department of Biology, Faculty of Biological Science, Urmia Branch, Islamic Azad University, Urmia, Iran.
Background: Colorectal cancer (CRC), now the second most prevalent malignant tumor worldwide, is more prevalent in young adults. In recent decades, there has been progress in creating anti-colorectal cancer medications, including cytotoxic compounds.
Objectives: Novel anticancer drugs are needed to surmount existing obstacles.
EJNMMI Res
March 2024
TUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, Garching, Germany.
Background: We recently introduced radiohybrid (rh)-based minigastrin analogs e.g., DOTA-rhCCK-18 (DOTA-D-Dap(p-SiFA)-(D-γ-Glu)-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH), that revealed substantially increased activity retention in the tumor.
View Article and Find Full Text PDFJ Nucl Med
January 2024
Department of Chemistry, Chair of Pharmaceutical Radiochemistry, TUM School of Natural Sciences, Technical University of Munich, Garching, Germany; and.
Because of the need for radiolabeled theranostics for the detection and treatment of medullary thyroid cancer (MTC), and the yet unresolved stability issues of minigastrin analogs targeting the cholecystokinin-2 receptor (CCK-2R), our aim was to address in vivo stability, our motivation being to develop and evaluate DOTA-CCK-66 (DOTA-γ-glu-PEG-Trp-(-Me)Nle-Asp-1-Nal-NH, PEG: polyethylene glycol) and DOTA-CCK-66.2 (DOTA-glu-PEG-Trp-(-Me)Nle-Asp-1-Nal-NH), both derived from DOTA-MGS5 (DOTA-glu-Ala-Tyr-Gly-Trp-(-Me)Nle-Asp-1-Nal-NH), and clinically translate [Ga]Ga-DOTA-CCK-66. Cu and Ga labeling of DOTA-CCK-66, DOTA-CCK-66.
View Article and Find Full Text PDFEJNMMI Res
July 2023
Department of Chemistry, Technical University of Munich, 85748, Garching, Germany.
Background: Over the last years, several strategies have been reported to improve the metabolic stability of minigastrin analogs. However, currently applied compounds still reveal limited in vitro and in vivo stability. We thus performed a glycine scan at the N-terminus of DOTA-MGS5 (DOTA-D-Glu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal) to systematically analyze the peptide structure.
View Article and Find Full Text PDFACS Appl Mater Interfaces
May 2023
Department of Oromaxillofacial-Head & Neck Oncology, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, College of Stomatology, National Center for Stomatology, National Clinical Research Center for Oral Diseases, Shanghai Key Laboratory of Stomatology, Shanghai Research Institute of Stomatology, Shanghai Jiao Tong University, Shanghai 200011, China.
Radiation-induced bone injury management remains a challenge in clinical practice, and there is no effective medicine. Recently, biomass-derived carbon dots (CDs) have attracted attention in biomedical engineering due to the advantages of abundant heteroatoms, low toxicity, and no need to drug loading. Here, we report that CDs, synthesized from via hydrothermal strategy, can effectively alleviate radiation-induced bone injury.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!