• In this study we designed and synthesized two ALK PROTACs

  2023-12-14

  

  In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci

• AhR is also known to cross talk with a

  2023-12-14

  

  AhR is also known to “cross-talk” with a variety of other cell signaling pathways, which has been the focus of a number of recent reviews [40], [41], [42]. It has long been known that TCDD is anti-estrogenic. For example, activation of AhR by TCDD and related HAHs inhibits estrogen dependent uterus

• valdecoxib synthesis br Material and methods br Results br D

  2023-12-14

  

  Material and methods Results Discussion GRK2 activity has increasingly been shown to contribute to the progression of numerous diseases and organ dysfunction [5], [6]. For instance, a large body of work over the last two decades has identified GRK2 as a major regulator of cardiac dysfunctio

• cyp450 inducers Role of APPL in endosomal signaling pathways

  2023-12-14

  

  Role of APPL in endosomal signaling pathways Endosomes consist of distinct membrane subdomains within individual organelles and assist in the translation of extracellular stimuli via cytoplasmic transduction cascades to the nucleus [3], [74]. Endosomal abnormalities are associated with the pathogen

• Lipotoxicity is the accumulation of excess lipids in non

  2023-12-14

  

  Lipotoxicity is the accumulation of excess lipids in non-adipose tissues that leads to cell dysfunction or cell death. It may play an important role in the pathogenesis of diabetes, and contributes to the rate of progression of CKD [7,8]. Emerging evidence indicates that renal lipid dysregulation is

• If overexpression of ADK is sufficient to induce spontaneous

  2023-12-14

  

  If overexpression of ADK is sufficient to induce spontaneous seizures, then reduction of ADK in engineered mice should prevent epileptogenesis. The generation of mice with moderately reduced levels of ADK in brain rather than complete ADK deficiency seems to be essential, since several lines of evid

• Molecular docking simulations were carried out for ligands

  2023-12-14

  

  Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Br

• However although in vitro studies in heterologous systems

  2023-12-14

  

  However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.

• br Identification of the kinase that phosphorylates

  2023-12-14

  

  Identification of the kinase that phosphorylates P450c17 The first Ser/Thr kinase that phosphorylates P450c17 was identified only recently. Of the 518 kinases in the human ‘kinome’ 278 are Ser/Thr kinases (Manning et al., 2002), but microarrays identified only 145 Ser/Thr kinases in human NCI-H29

• br Apelin The APJ receptor ligand apelin firstly

  2023-12-13

  

  Apelin The APJ receptor ligand apelin firstly in 1998 was segregated from bovine stomach tissue. Human preproapelin gene located on chromosome Xq25–26.1. The apelin preproproteins consist of 77 amino Ro 3306 residues that are cleaved into biologically active C-terminal fragments of various sizes

• Although little is known about

  2023-12-13

  

  Although little is known about the etiopathogenesis of preeclampsia, this syndrome has a major impact on maternal and fetal health worldwide, since it is responsible for 10–15% of maternal deaths [16], [17], preterm births, intrauterine growth restriction (IUGR), and fetal deaths [2]. In developing

• influenza m2 protein br Author Contributions br Acknowledgme

  2023-12-13

  

  Author Contributions Acknowledgments Introduction Cerebral ischemia-reperfusion (I/R) injury is a pathological phenomenon that occurs after restoration of blood supply to influenza m2 protein tissues subsequent to ischemia or hypoxia (Carden and Granger, 2000). It typically occurs after the

• Because activation of HT A

  2023-12-13

  

  Because activation of 5-HT2A receptor is capable of facilitating dopamine cell activity and dopamine release (Bortolozzi et al., 2003), and this action of dopamine is known to mediate rat maternal behavior, especially maternal motivation (Afonso et al., 2007, Febo et al., 2010, Li and Fleming, 2003,

• br Introduction In myasthenia gravis

  2023-12-13

  

  Introduction In myasthenia gravis (MG), autoantibodies against the native AChR conformation cause loss of AChR at the neuromuscular junction and fatigable muscle weakness (Newsom-Davis et al., 1993). The AChR is a pentameric transmembrane protein, with two splice forms of the α-subunit, P3A− and

• br Dihydrotestosterone in adult fish

  2023-12-13

  

  Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance

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