Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics
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Isocitrate lyase (ICL) plays a pivotal role in the persistence of Mycobacterium tuberculosis in mice by sustaining intracellular infection in inflammatory macrophages. The enzyme allows net carbon gain by diverting acetyl-CoA from beta-oxidation of fatty a ...
The intracellular fatty acid content of insulin-sensitive target tissues determines in part their insulin sensitivity. Uptake of fatty acids into cells is a controlled process determined in part by a regulated import/export system that is controlled at lea ...
Protoporphyrin IX (PpIX) is used as a fluorescence marker and photosensitizing agent in photodynamic therapy (PDT). A temporary increase of PpIX in tissues can be obtained by administration of 5-aminolevulinic acid (ALA). Lipophilicity is one of the key pa ...
Uptake of fatty acids into cells is a controlled process in part regulated by fatty acid transport proteins (FATPs), which facilitate the transport of fatty acids across the cell membrane. In this study the structure of the human FATP-1 (HGMW-approved symb ...
Cyclo-beta-tetrapeptide I, a beta-peptidic analog of octreotide, was prepd. from beta-amino acid building blocks synthesized by Arndt-Eistert homologation of appropriately protected alpha-amino acids. The affinity of I for five different human somatostatin ...
The three types of peroxisome proliferator activated receptor (PPAR), alpha, beta (or delta), and gamma, each with a specific tissue distribution, compose a subfamily of the nuclear hormone receptor gene family. Although peroxisome proliferators, including ...
A rapid synthesis of aryl triflate and aryl nonaflate was developed using 4-nitrophenyl triflate and 4-nitrophenyl nonaflate as perfluoroalkanesulfonyl transfer reagents in combination with polymer supported 1,5,7-triazabicyclo[4.4.0]dec-5-ene (PTBD). Simp ...
LXR alpha (liver X receptor, also called RLD-1) is a nuclear receptor, highly expressed in tissues that play a role in lipid homeostasis. In this report we show that fatty acids are positive regulators of LXR alpha gene expression and we investigate the mo ...
It is currently thought that the effects of PPARgamma activation on glucose homeostasis may be due to the effect of this nuclear receptor on the production of adipocyte-derived signalling molecules, which affect muscle glucose metabolism. Potential signall ...
Solid phase syntheses of the OF4949 derivs. I (R = H, CH2CONH2) and II (R1 = H, R2 = H, NH2; R1 = NH2, R2 = H) were performed via protection/deprotection of tyrosine side chains on a support, and SNAr macrocyclization reactions. [on SciFinder (R)] ...
