• GnRH ant have been designed

  2022-01-03

  

  GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p

• Percentage contribution to free glutamate intake was

  2022-01-03

  

  Percentage contribution to free glutamate intake was also calculated at the food item level. A list of the top 30 foods for children and adults are presented separately in Table 2. The top 4 foods included in this list are watermelon, raw; tomato catsup; tomatoes, raw; and roll, white, soft. These a

• Introduction Human pathogenic Leishmania protozoa comprise

  2022-01-03

  

  Introduction Human pathogenic Leishmania protozoa comprise 20 different species that are distributed throughout the world and cause the disease leishmaniasis [1]. Transmission primarily occurs through the bite of a female sand fly and clinical manifestations of the disease span from cutaneous lesio

• br Acknowledgments This work was funded by

  2022-01-03

  

  Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa

• Attempting to further elucidate the role of

  2022-01-03

  

  Attempting to further elucidate the role of stat3 inhibitor and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as β cell area

• Beside these studies related to food

  2022-01-03

  

  Beside these studies related to food, several groups examined the role of ghrelin in the actions of psychostimulants. Modulation of the ghrelin system and food restriction alter locomotor sensitization, DA release in the NAc, and CPP induced by cocaine, amphetamine, and nicotine (Abizaid et al., 201

• Previously we have shown that ghrelin and cannabinoids stimu

  2022-01-03

  

  Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo

• A comparison of our results with literature data on the

  2022-01-03

  

  A comparison of our results with literature data on the action of pregnane and androstane steroids on the functional activity of NMDAR, GABAAR and GlyR enables us to draw the following conclusions. First, androstane steroids (with no substituents at C-17) at a concentration up to 50 μM do not affect

• In perimenstrual catamenial epilepsy there is emerging evide

  2022-01-03

  

  In perimenstrual catamenial epilepsy, there is emerging evidence to suggest that P withdrawal plays a key role in seizure exacerbations occurring around the time of menstruation (Backstrom et al., 1984, Bonuccelli et al., 1989, Scharfman and MacLusky, 2006). The mechanisms underlying ovarian cycle-r

• To understand the structural basis for

  2022-01-03

  

  To understand the structural basis for the mode of action of indole-based compounds the crystal structures of bound to both the wild type and A128T IN CCDs have been solved. The X-ray crystallography studies have revealed that binds at the IN dimer interface in the principal LEDGF/p75 binding pocket

• Chicoric acid CA is a di acylated hydroxycinnamoyl tartaric

  2022-01-03

  

  Chicoric YM 58483 receptor (CA) is a di-acylated hydroxycinnamoyl tartaric acid ester [12] found in a variety of plant species, especially within the Astereceae family [13]. Of interest for this study, Sonchus oleraceus and Bidens pilosa plants, from Astereceae family, were used. Both S. oleraceus a

• br Conflicts of interest br

  2022-01-03

  

  Conflicts of interest Significance p53 is required for the induction of cell senescence to limit the proliferation of polyploid cells. We found that Hippo signal deficiency or Yap activation in mouse livers result in polyploid formation and polyploid cell growth. The combined loss of Hippo sig

• Amrubicin Given the overexpression of HO in some tumors such

  2022-01-03

  

  Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho

• PLP has been found to be

  2021-12-31

  

  PLP has been found to be effective inhibitor of many enzymes that have sodium channel for phosphate-containing substrates or effectors, including RNA polymerase [14], [15], reverse transcriptase [16], and DNA polymerase [17], [18]. Oka et al. [19], [20] reported that vitamin B6 deficiency generally

• While the specific set of challenges associated

  2021-12-31

  

  While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav

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