538-37-4Relevant articles and documents
Novel antibody-antibiotic conjugate eliminates intracellular S. aureus
Lehar, Sophie M.,Pillow, Thomas,Xu, Min,Staben, Leanna,Kajihara, Kimberly K.,Vandlen, Richard,DePalatis, Laura,Raab, Helga,Hazenbos, Wouter L.,Hiroshi Morisaki,Kim, Janice,Park, Summer,Darwish, Martine,Lee, Byoung-Chul,Hernandez, Hilda,Loyet, Kelly M.,Lupardus, Patrick,Fong, Rina,Yan, Donghong,Chalouni, Cecile,Luis, Elizabeth,Khalfin, Yana,Plise, Emile,Cheong, Jonathan,Lyssikatos, Joseph P.,Strandh, Magnus,Koefoed, Klaus,Andersen, Peter S.,Flygare, John A.,Wah Tan, Man,Brown, Eric J.,Mariathasan, Sanjeev
, p. 323 - 328 (2015)
Staphylococcus aureus is considered to be an extracellular pathogen. However, survival of S. aureus within host cells may provide a reservoir relatively protected from antibiotics, thus enabling long-term colonization of the host and explaining clinical f
Investigating the role of the geminal dimethyl groups of coenzyme A: Synthesis and studies of a didemethyl analogue
Vogel, Kurt W.,Stark, Lucy M.,Mishra, Pranab K.,Yang, Wei,Drueckhammer, Dale G.
, p. 2451 - 2460 (2000)
An analogue 2 of coenzyme A (CoA) has been prepared in which the geminal methyl groups are replaced with hydrogens. An NMR titration study was conducted and shifts in frequency of protons in the pantetheine portion of the molecule upon titration of the adenine base were observed as has been previously reported with CoA. These studies indicate that the geminal dimethyl groups are not essential for adoption of a partially folded conformation in solution. Based on 1H-1H coupling constants, the distribution of conformations about the carbon-carbon bonds in the region of the methyl deletion were estimated. The results suggest that the conformer distribution is similar to that of CoA, but with small increases in population of the anti conformers. A simple model compound containing the didemethyl pantoamide moiety was prepared and subjected to similar conformational analysis. The coupling constants and predicted conformer distribution were almost identical to that of the CoA analogue, indicating that the conformer distribution is controlled by local interactions and not influenced by interactions between distant parts of the CoA molecule. The acetyl derivative of 2 was a fairly good substrate for the acetyl-CoA utilizing enzymes carnitine acetyltransferase, chloramphenicol acetyltransferase, and citrate synthase, with 1.3- to 10-fold increased K(m) values and 2.5- to 11-fold decreases in V(max). The combined results indicate that the geminal dimethyl groups of CoA have modest effects on function and minimal effects on conformation. Copyright (C) 2000 Elsevier Science Ltd.
METHODS AND COMPOSITIONS FOR PRODRUG FORMS OF SPECTINOMYCIN AND SPECTINAMIDE ANALOGS
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Paragraph 0589-0590; 0602; 0609; 0615; 0621, (2020/06/01)
In one aspect, the disclosure relates to substituted spectinomycin analogs, including substituted aminomethyl spectinomycin analogs and substituted spectinamide analogs, with increased tolerability and safety, including improved tolerability to parenteral
COMPOSITIONS COMPRISING ENZYME CLEAVABLE LINKER PLATFORMS AND CONJUGATES THEREOF
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Page/Page column 71; 72, (2021/01/23)
The present invention relates to a cleavable linker platform. In particular, the invention relates to construction of an enzyme cleavable linker platform conjugated to a drug or a diagnostically relevant compound, a biomolecule, and an enzyme cleavable group, for which cleavage of the enzyme cleavable group leads to release of the drug or diagnostically relevant compound.