• cAMP mediated signaling pathways are important for maintaini

  2019-12-09

  

  cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, BWX 46 of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased expression of un

• br Oxidoreductase like MEM for prodrug activation br Future

  2019-12-09

  

  Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2

• Introduction Obesity constitutes a global healthcare

  2019-12-09

  

  Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV

• br Results br Discussion Thus the biochemical and

  2019-12-09

  

  Results Discussion Thus, the biochemical and structural studies of six Maf proteins from different organisms have revealed two subfamilies of new enzymes with the metal-dependent nucleoside triphosphate pyrophosphatase activity against both canonical and noncanonical pyrimidine nucleotides (Yh

• It has been reported that NMDA receptor hypofunction upregul

  2019-12-09

  

  It has been reported that NMDA receptor hypofunction upregulates the expression of immediate early genes in several 350 mg regions [39], [40]. Consistent with this finding, we demonstrated that MK-801 increased the number of c-Fos-positive cells in the PVN and PC/RS (Fig. 5). Importantly, the MK-80

• Several highly selective COX inhibitors

  2019-12-09

  

  Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d

• br Acknowledgements br A subgroup of pediatric solid

  2019-12-06

  

  Acknowledgements A subgroup of pediatric solid neoplasms, collectively referred to as small round cell tumors (SRCTs) of childhood, demonstrates undifferentiated small round cell morphological characteristics. The SRCTs include neuroblastomas, lymphomas, and several bone and soft tissue sarcoma

• br Results br Discussion In this paper we

  2019-12-06

  

  Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 mirtazapine high via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1

• At first cartilage damage in osteoarthritis reflects the los

  2019-12-06

  

  At first, cartilage damage in osteoarthritis reflects the loss of proteoglycan and collagen network that increases the swelling of tissues. The incremented expression of DDR2 receptor has also co-related with the depletion of cartilage in surgically induced OA model [8]. Osteoarthritis, a degenerati

• br Acknowledgements br Introduction Three structurally relat

  2019-12-06

  

  Acknowledgements Introduction Three structurally related fungal metabolites have been isolated from chloroform extracts of submerged rice cultures of Aspergillus terreus 23-1 from stored unhulled rice in Taiwan; these were named territrems A–C to indicate their biological origin (A. terreus) a

• Advances in the total chemical synthesis of ubiquitin have e

  2019-12-06

  

  Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio

• In this context we initiated

  2019-12-06

  

  In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in U-73122 replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structura

• In this study we have developed and investigated three

  2019-12-06

  

  In this study we have developed and investigated three NADPH-regenerating fusion partners with two different enzyme systems: a BVMO and an ADH. With the exception of one fusion construct (StGDH with LbADH), all fusion PFK-015 resulted in good soluble expression as well as fully functional as self-s

• CYP s are heme containing monooxygenases constituting a cons

  2019-12-06

  

  CYP450s are heme-containing monooxygenases constituting a conserved gene superfamily of heme-thiolate proteins, and are found in prokaryotes and eukaryotes (Martignoni et al., 2006). They play a key role in detoxification of endogenous (e.g., steroids) and exogenous compounds (e.g., drug, insecticid

• br Crystal structure of c

  2019-12-06

  

  Crystal structure of c-FMS and binding pattern of CSF-1 and IL-34 c-FMS is a 972 amino acids polypeptides containing transmembrane glycoprotein [19]. It contains all the necessary domains required for tyrosine kinase activity, i.e. 512 amino 3-Deazaneplanocin N-terminal extracellular segment, hyd

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