The synthesis of new N1,N8-diacetylspermidine (DiAcSpd) analogues having a linker with desired functional groups in the methylene skeleton, which have been designed by theoretical calculations, is described. We have also achieved the preparation of DiAcSpd supported on solid-phase resins, which have the potential to be used for the evolution of ligands by exponential enrichment (SELEX).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1039/c8ob02900h | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Nitric oxide transfer between nominal Fe and Co biomimetics of the nitrile hydratase active site.
J Biol Inorg Chem
January 2025
Department of Chemistry, Texas A&M University, College Station, TX, 77843, USA.
Related to the inactive form of nitrile hydratase, NHase, that contains Fe(NO) within tripeptide NS binding environment, the NO transfer reactivity of (bis-mercaptoethane diazacycloheptane)Fe(NO) and (bis-mercaptoethane diazadimethylethane)Fe(NO) is compared to Co(NO) analogs. Acceptors of NO include cobalt octaethylporphyrin and the [(NS)M] dimeric precursors in the synthesis of the Fe(NO) and Co(NO) biomimetics. Qualitative rates are augmented by a definitive kinetic study finding that rates of NO transfer from (NS)M(NO) to [(NS)M'] are dependent on M and M' as well as the hydrocarbon N to N and N to S linkers.
View Article and Find Full Text PDFPhotoluminescent Properties of Tb-UiO-66 Metal-Organic Framework Analogues.
Inorg Chem
January 2025
Department of Chemistry and Biochemistry and Centre for NanoScience Research, Concordia University, 7141 Sherbrooke Street West, Montreal, Quebec H4B 1R6, Canada.
Three new analogues of Tb-UiO-66 with various functional groups (-F, -Br, -NH) on the terephthalic acid linker of the metal-organic framework (MOF) are synthesized and characterized. The photoluminescent properties of these analogues, as well as Tb-UiO-66 and Tb-UiO-66-(OH), are studied and correlated to the calculated energies for the triplet (T) states of each linker. The results show that the addition of electron withdrawing groups, such as -F and -Br, lead to higher T energies, resulting in quantum yields in the range of 6-31%.
View Article and Find Full Text PDFDegrading the key component of the inflammasome: development of an NLRP3 PROTAC.
Chem Commun (Camb)
January 2025
Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
This study explores PROTACs for NLRP3, the key player in innate immunity. We utilised a thiophene analogue of the NLRP3 inhibitor MCC950 and employed CuAAC chemistry for the assembly of PROTACs bearing various linkers and recruiting three different E3 ligases. Compounds were evaluated in bidirectional thermal stability studies with NLRP3 and E3 ligases.
View Article and Find Full Text PDFReducing the Formation of Toxic Byproducts During the Photochemical Release of Epinephrine.
J Xenobiot
January 2025
Department of Physics, Novosibirsk State University, 630090 Novosibirsk, Russia.
Engineered light-sensitive molecules offer a sophisticated toolkit for the manipulation of biological systems with both spatial and temporal precision. Notably, artificial "caged" compounds can activate specific receptors solely in response to light exposure. However, the uncaging process can lead to the formation of potentially harmful byproducts.
View Article and Find Full Text PDFThe validation and clinical bioanalysis of the Bicycle® Toxin Conjugate zelenectide pevedotin in human plasma.
Bioanalysis
January 2025
Quantitative Pharmacology, Bicycle Therapeutics, Cambridge, MA, USA.
Background: The Bicycle® toxin conjugate (BTC) zelenectide pevedotin, formerly known as BT8009, is a novel bicyclic peptide targeting the Nectin-4 tumor antigen conjugated to the cytotoxin monomethyl auristatin E (MMAE) via a valine-citrulline cleavable linker. Zelenectide pevedotin is currently being investigated in a Phase 1/2 (Duravelo-1, NCT04561362) clinical trial to determine safety and efficacy in patients with tumors associated with Nectin-4 expression. A simple regulated bioanalytical assay was developed to quantify intact zelenectide pevedotin in patient plasma samples.
View Article and Find Full Text PDFWant 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!