Incretin mimetics are set to become a mainstay of type 2 diabetes treatment. By acting on the pancreas and brain, they potentiate insulin secretion and induce weight loss to preserve normoglycemia. Despite this, incretin therapy has been associated with off-target effects, including nausea and gastrointestinal disturbance. A novel photoswitchable incretin mimetic based upon the specific glucago...

Merocyanine (MC) isomers that are formed after absorption of a UV photon by 1',3'-dihydro-1',3'-3'-trimethyl-6-nitrospiro[2H-1-benzopyran-2',2'-(2H)-indole] were studied. Several, predominantly TTC and TTT, merocyanine isomers are present in toluene solution ("T" and "C" indicate trans and cis conformations of the C-C bonds in the methine bridge). Excitation in the MC visible absorption band (a...

Platinum-based anticancer drugs act therapeutically by forming DNA adducts, but suffer from severe toxicity and resistance problems, which have not been overcome in spite of decades of research. And yet defined chromatin targets have generally not been considered in the drug development process. Here we designed novel platinum-intercalator species to target a highly deformed DNA site near the n...

In presence of oleate and taurocholate, differentiated CaCo-2 cell monolayers on membranes were able to assemble and secrete chylomicrons. Under these conditions, both cellular uptake and secretion into chylomicrons of beta-carotene (beta-C) were curvilinear, time-dependent (2-16 h), saturable, and concentration-dependent (apparent K(m) of 7-10 microM) processes. Under linear concentration cond...

In summary, we presented a design strategy for chiral, amphiphilic, and photoswitchable molecule, using cholesterol, sulfonate, cyanostilbene. The molecule could self-assemble to the trans-isomer in aqueous solution, which is accompanied by strong CD signals. Both trans- cis-isomers are thermally stable, high conversion photoswitching between with good fatigue resistance reversibility, can be a...

5,6-trans-AA (5,6-TAA, where TAA stands for trans-arachidonic acid) is a recently identified trans fatty acid that originates from the cis-trans isomerization of AA initiated by the NO2 radical. This trans fatty acid has been detected in blood circulation and we suggested that it functions as a lipid mediator of the toxic effects of NO2. To understand its role as a lipid mediator, we studied th...

While the catalytic activity of some Ru-based polypyridine complexes in water oxidation is well established, the relationship between their chemical structure and activity is less known. In this work, the single site Ru complex [Ru(bpy)2(H2O)2] (bpy = 2,2′-bipyridine)—which can exist as either a cis isomer or a trans isomer—is investigated. While a difference in the catalytic activity of these ...

Equilibrium constants for the mercuric acetate-catalyzed been determined in the liquid and vapor phase over the temperature range 30 ° 175 °C by gas chromatography analysis. A novel synthesis of the cisand trans-isomers of l,2-dimethoxyethylene is discussed. From a screening of 29 catalysts, mercuric acetate, mercuric benzoate, and mercuric salicylate were found to be favorable isomerization ca...

Anabaena Sensory Rhodopsin (ASR) stands out among the microbial retinal proteins in that, under light-adaptation (LA) conditions, it binds both the 13-cis isomer and the all-trans isomer of the protonated Schiff base of retinal (PSBR). In the dark-adapted (DA) state, more than 95% of the proteins bear all-trans PSBR, and the protein environment adopts a different equilibrium state. We report th...

by Rieche et al. (1). These compounds are also referred to as monomeric ozonides, but this terminology appears to be a misnomer. Hence, the term ozonide is used for “true ozonides” in the present study. During the course of our studies, Schroder (2 ) reported the formation of cisand trans-isomeric ozonides on the ozonization of cis-di-t-butylethylene. Only the trans-isomer was detected on the o...