Gene/Protein Disease Symptom Drug Enzyme Compound
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The presence of proteoglycans (PGs) was studied in compact lamellar rat and human bone at the electron microscopic level. With the cationic dye cuprolinic blue (CB1), PGs could be demonstrated in the mineralized bone matrix. The amounts of PGs appeared to be equal in the different lamellae and osteons. More CBl-positive material was found in the outermost lamella of the cortex, in the perilacunar matrix around the osteocyte lacunae, and around the canaliculi. Enzyme digestion with chondroitinase ABC demonstrated that the CBl-positive rods consisted of PGs. These observations amplify biochemical studies in which PGs have been isolated from the mineralized bone matrix. The presence of CBl-positive rods in the mineralized matrix suggest that PGs do not have to be removed completely to make the matrix calcifiable.
Anat Rec 1992 Jan
PMID:An electron microscopic study on the presence of proteoglycans in the mineralized matrix of rat and human compact lamellar bone. 153 63

Methods for the preparation of II-VI, III-V, and II-V as well as other compound semiconductor nanoparticles using main group single-molecular precursors have been developed. The work involves the design and synthesis of compounds containing all the elements required within the desired nanoparticulate material. Precursors are tailored to give reproducible, clean decomposition at moderate temperatures, leading to high quality, defect free, mono-dispersed nanoparticles. In this article we cover key aspects of precursor and nanoparticle synthesis. One of the more successful and reproducible series of single-source precursors used, and the one on which we have concentrated our research efforts, is the bis(dialkyldithio-/diseleno-carbamato)cadmium(II)/zinc(II) compounds, M(E(2)CNR(2))(2) (M = Zn or Cd, E = S or Se, and R = alkyl) for the preparation of chalcogenide nanoparticulate materials. Preliminary mechanistic studies suggest that the precursor to nanoparticle deposition route is strongly influenced by the alkyl substituent groups present, and may well determine the phase and quality of the final metal chalcogenide nanoparticles produced. Herein we discuss the synthesis of semiconductor nanoparticles using such single-molecular precursors.
Chem Rec 2001
PMID:Syntheses of semiconductor nanoparticles using single-molecular precursors. 1193 52

The observed antiobesity effect of rimonabant (1) in a pharmacological rodent model 10 years ago has led to a surge in the search for novel cannabinoid CB1 antagonists as a new therapeutic target for the treatment of obesity. Rimonabant showed clinical efficacy in the treatment of obesity and also improved cardiovascular and metabolic risk factors. Cannabinoid CB1 receptor antagonists have also good prospects in other therapeutic areas, including smoking and alcohol addiction as well as cognitive impairment. Solvay's research achievements in this fast-moving field are reported in relation with the current state of the art. Several medicinal chemistry strategies have been pursued. The application of the concept of conformational constraint led to the discovery of more rigid analogs of the prototypic CB1 receptor antagonist rimonabant. Replacement of the central heterocyclic pyrazole ring in rimonabant yielded imidazoles, triazoles, and thiazoles as selective CB1 receptor antagonists. Dedicated medium-throughput screening efforts delivered one 3,4-diarylpyrazoline hit. Its poor pharmacokinetic properties were successfully optimized which led to the discovery of orally active and highly CB1/CB2 receptor selective analogs in this series. Regioisomeric 1,5-diarylpyrazolines, 1,2-diarylimidazolines, and water-soluble imidazoles have been designed as novel CB1 receptor antagonist structure classes.
Chem Rec 2008
PMID:Cannabinoid CB1 receptor antagonists in therapeutic and structural perspectives. 1856 99

Recently, the endocannabinoid (EC) system and the presence of CB1 receptor (CB1-R), have been identified in human sperm. However, the effects of EC receptor ligands such as anandamide (N-arachidonoylethanolamine) and the role of EC system in male fertility is still largely unexplored. In the present study, we investigated the ultrastructural compartmentalization of CB1-R and analyzed the effects of its stimulation by using a stable analog of anandamide, 2-methylarachidonyl-2'-fluoro-ethylamide (MET-F-AEA). We focused particularly on sperm survival and acrosin activity. The study of human sperm anatomy by transmission electron microscopy with immunogold analysis revealed the location of the CB1-R prevalently in the sperm membranes of the head and interestingly on the mitochondria. The effect of different concentrations of MET-F-AEA from 100 nM to 1 microM evidenced a significant decrease of sperm survival. Interestingly, we analyzed this negative effect at molecular level, testing the EC action on different known sperm survival targets. MET-F-AEA-treatment decreased both pBCL2 and pAkt, two prosurvival proteins, and increased pPTEN expression which is the main regulator of the PI3K/Akt pathway. Moreover, a biphasic effect was observed with increasing MET-F-AEA concentrations on the acrosin activity. The blockage of the CB1-R by using its selective antagonist SR141716 (rimonabant) induced an opposite action on sperm survival supporting a role for this receptor in the biology of the male gamete.
Anat Rec (Hoboken) 2010 Feb
PMID:Human sperm anatomy: ultrastructural localization of the cannabinoid1 receptor and a potential role of anandamide in sperm survival and acrosome reaction. 1993 10