• Two critical determinants of receptor trafficking are

  2023-08-11

  

  Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al

• Several structural classes of ASK inhibitors mostly from

  2023-08-11

  

  Several structural p m x of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revealed s

• br ASK in Huntington s disease and

  2023-08-11

  

  ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production

• Furthermore we also found that the basic level of

  2023-08-11

  

  Furthermore, we also found that the basic level of ROS was markedly lower in mtDNA-reduced SW480 MG0103 than that in the parent cells. Endogenous ROS is most notably produced at the sites of complex I and complex III [5], it might be plausible that the decreased quantity of ROS observed in mtDNA-re

• Thiazole heterocycles constitute an interesting class of mol

  2023-08-11

  

  Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.

• br Small molecule homoisoflavonoid in combination

  2023-08-11

  

  Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m

• br Summary and future br Introduction Androgen activity is c

  2023-08-11

  

  Summary and future Introduction Androgen activity is critical for a wide range of developmental and physiological responses and is especially important in male sexual differentiation and maturation. The biological activity of androgens occurs through binding to the androgen receptor (AR) and t

• Introduction Aldose reductase ALR is

  2023-08-11

  

  Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr

• Thus far clinical data indicate that IDO inhibitors have man

  2023-08-11

  

  Thus far, clinical data indicate that IDO1 inhibitors have manageable toxicity, albeit with a relatively short period of treatment in a small number of patients. KYN is a pluripotent mediator and key intermediate for the synthesis of a host of downstream KP metabolites that are implicated in inflamm

• Application of the broad acting

  2023-08-11

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• Since the introduction of zebrafish into the laboratory many

  2023-08-11

  

  Since the introduction of zebrafish into the laboratory, many milestones have been achieved that firmly establish this organism as a prominent genetic model for biology and medicine. Many features make this species an organism of easy maintenance in laboratory which provides advantages to understand

• In pioneering work from Ikeda and colleagues

  2023-08-11

  

  In 2006, pioneering work from Ikeda and colleagues showed that GMF localizes to and regulates the iox cytoskeleton (see Glossary), and noted its sequence similarity to ADF/cofilin[11]. In 2009, the structure of GMF [6] was solved, revealing it to be a bona fide member of the actin depolymerizing fa

• br GMF Remodels Actin Networks

  2023-08-11

  

  GMF Remodels Actin Networks at the Leading Edge How are the conserved activities of GMF used in vivo to regulate branched Linifanib networks (e.g., at sites of endocytosis and at the leading edge) (Figure 2A,B)? In animal cells, the regulatory effects of GMF on actin networks appear to govern la

• br Acknowledgements MC and PD were funded by the Michael

  2023-08-11

  

  Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b

• Fig A shows a schematic representation

  2023-08-11

  

  Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the

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