scholarly journals The fate of P2Y-related orphan receptors: GPR80/99 and GPR91 are receptors of dicarboxylic acids

2004 ◽  
Vol 1 (1) ◽  
pp. 17-20 ◽  
Author(s):  
Nathalie Suarez Gonzalez ◽  
Didier Communi ◽  
Sébastien Hannedouche ◽  
Jean-Marie Boeynaems
Keyword(s):  
Dicarboxylic Acids ◽  
Orphan Receptors

Chemically Fueled Assembly of Macrocycles Comprising Multiple Transient Bonds

2019 ◽  
Author(s):  
Mohammad Mosharraf Hossain ◽  
Joshua Atkinson ◽  
Scott Hartley
Keyword(s):  
Covalent Bond ◽  
Dicarboxylic Acids ◽  
Molecular Assembly ◽  
Chemical Systems ◽  
Complex Architectures ◽  
The Creation ◽  
Dynamic Exchange

Dissipative (nonequilibrium) assembly powered by chemical fuels has great potential for the creation of new adaptive chemical systems. However, while molecular assembly at equilibrium is routinely used to prepare complex architectures from polyfunctional monomers, species formed out of equilibrium have, to this point, been structurally very simple. In most examples the fuel simply effects the formation of a single transient covalent bond. Here, we show that chemical fuels can assemble bifunctional components into macrocycles containing multiple transient bonds. Specifically, dicarboxylic acids give aqueous dianhydride macrocycles on treatment with a carbodiimide. The macrocycle is assembled efficiently as a consequence of both fuel-dependent and -independent mechanisms: it undergoes slower decomposition, building up as the fuel recycles the components, and is a favored product of the dynamic exchange of the anhydride bonds. These results create new possibilities for generating structurally sophisticated out-of-equilibrium species.

Chemically Fueled Assembly of Macrocycles Comprising Multiple Transient Bonds

2019 ◽  
Author(s):  
Mohammad Mosharraf Hossain ◽  
Joshua Atkinson ◽  
Scott Hartley
Keyword(s):  
Covalent Bond ◽  
Dicarboxylic Acids ◽  
Molecular Assembly ◽  
Chemical Systems ◽  
Complex Architectures ◽  
The Creation ◽  
Dynamic Exchange

Dissipative (nonequilibrium) assembly powered by chemical fuels has great potential for the creation of new adaptive chemical systems. However, while molecular assembly at equilibrium is routinely used to prepare complex architectures from polyfunctional monomers, species formed out of equilibrium have, to this point, been structurally very simple. In most examples the fuel simply effects the formation of a single transient covalent bond. Here, we show that chemical fuels can assemble bifunctional components into macrocycles containing multiple transient bonds. Specifically, dicarboxylic acids give aqueous dianhydride macrocycles on treatment with a carbodiimide. The macrocycle is assembled efficiently as a consequence of both fuel-dependent and -independent mechanisms: it undergoes slower decomposition, building up as the fuel recycles the components, and is a favored product of the dynamic exchange of the anhydride bonds. These results create new possibilities for generating structurally sophisticated out-of-equilibrium species.

INFLUENCE OF DICARBOXYLIC ACIDS ON SOWING QUALITY OF SPRING BARLEY

1970 ◽  
pp. 22-25
Author(s):  
N. N. Loy ◽  
S. N. Gulina
Keyword(s):  
Organic Acids ◽  
Spring Barley ◽  
Dose Range ◽  
Dicarboxylic Acids ◽  
Rotary Machine ◽  
Working Solution ◽  
Negative Effect ◽  
Sprouted Seeds

The effect of presowing seed treatment on various concentrations of dicarboxylic (organic) acids on the sowing characteristics of spring barley has been studied. Seeds were treated with organic acids obtained by exposing cuttings to the radiation with a dose of 100 kGy and consequent hydrolysis, in concentrations: 1•10-7 %; 1•10-9; 1•10-11; 1•10-13 and 1•10-15 % on a laboratory rotary machine RVO-64 for one day before laying for germination. Distilled water was used for the control case. The rate of application of the working solution calculated as 10 liters / ton of seeds. Seeds were germinated in filter paper rolls in accordance with GOST 12038-84 requirements. The temperature was maintained at +24 ° C in the thermostat where the glasses with rolls were placed. For determination of germinative power and laboratory germination the sprouted seeds were evaluated after three and seven days, respectively. In laboratory experiments it was established that the treatment of barley seeds of varieties Zazersky 85, Nur and Vladimir with organic acids (OK) in different concentrations had both a stimulating and a negative effect. On the Zazersky 85 variety, in variants with acid concentrations of 1•10-9 and 1•10-11, an increase in germination energy (EP) by 2-4% and a significant decrease (by 3-4%) of laboratory germination (LV) of barley seeds were noted. On the Nur variety, the increase in EP was observed at 4% (concentration 1•10-11), LV and seed growth force (CPC) by 2-7% at a concentration of 1•10-7 and in the dose range 1•10-11 - 1•10-14 compared to the control values. On the grade of Vladimir, an increase in EP, LV, and CPC was found to increase by 1-6% at concentrations OK 1•10-7 and 1•10-13. It was shown that the treatment of seeds with acids led to an increase in the length of the germ in all studied varieties (by 3-9%) and dry biomass of 7-day-old seedlings - by 3-6%. Consequently, the treatment of seeds with a mixture of dicarboxylic acids has a stimulating effect on the sowing quality of spring barley.

Molecular Modeling of an Orphan GPR18 Receptor

2019 ◽  
Vol 16 (10) ◽  
pp. 1167-1174 ◽  
Author(s):  
Kamil J. Kuder ◽  
Tadeusz Karcz ◽  
Maria Kaleta ◽  
Katarzyna Kiec-Kononowicz
Keyword(s):  
Cannabinoid Receptors ◽  
Cannabinoid Receptor ◽  
Glycine Receptor ◽  
Homology Model ◽  
Orphan Receptor ◽  
Receptor Ligands ◽  
Orphan Receptors ◽  
Inactive Form ◽  
Starting Point ◽  
Endogenous Cannabinoid

Background: : One of the best known to date GPCR class A (Rhodopsin) includes more than 100 orphan receptors for which the endogenous ligand is not known or is unclear. One of them is N-arachidonyl glycine receptor, named GPR18, a receptor that has been reported to be activated by Δ9-THC, endogenous cannabinoid receptors agonist anandamide and other cannabinoid receptor ligands suggesting it could be considered as third cannabinoid receptor. GPR18 activity, as well as its distribution might suggest usage of GPR18 ligands in treatment of endometriosis, cancer, and neurodegenerative disorders. Yet, so far only few GPR18 antagonists have been described, thus only ligand-based design approaches appear to be most useful to identify new ligands for this orphan receptor. Methods: : Main goal of this study, GPR18 inactive form homology model was built on the basis of the evolutionary closest homologous template: Human P2Y1 Receptor crystal structure. Results: : Obtained model was further evaluated and showed active/nonactive ligands differentiating properties with acceptable confidence. Moreover, it allowed for preliminary assessment of proteinligand interactions for a set of previously described ligands. Conclusion:: Thus collected data might serve as a starting point for a discovery of novel, active GPR18 blocking ligands.

The synthesis of model lactones of cyclolignan type

1981 ◽  
Vol 46 (9) ◽  
pp. 2123-2128 ◽  
Author(s):  
Jiří Křepelka ◽  
Jiří Holubek
Keyword(s):  
Sodium Borohydride ◽  
Catalytic Hydrogenation ◽  
Dicarboxylic Acids ◽  
Inhibitory Effect ◽  
Experimental Animals

Lactones VI-IX were prepared on reduction of anhydrides of 4-aryl-1-methoxynaphthalene-2,3-dicarboxylic acids IV and V with sodium borohydride in methanol. Catalytic hydrogenation on platinum of lactones VIII and IX gave lactones with hydrogenated ring A, or A and C. Lactones XII and XIII were found to possess an inhibitory effect on the growth of the tumour S 37 in experimental animals.

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