• From an historical perspective ligands

  2024-04-01

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, punicalagin mg or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands

• br Discussion br Acknowledgments Writing

  2024-04-01

  

  Discussion Acknowledgments Writing of this review and collection of data from our laboratories that are presented were supported by a grant from the Belgian Science Policy (BELSPO) SSTC Interuniversity Attraction Poles Plastoscine P7/17 to AVDL and JB, multiple grants from the Fund for Scienti

• In the present study a splice acceptor

  2024-03-30

  

  In the present study, a splice acceptor site mutation (c.1769-1G > C) was identified in AR gene from patients with CAIS. The c.1769-1G > C mutation results in replacement of the normal sequence (CAG/G) with a new sequence (CAC/G) at the splice acceptor site of intron 2. In the splice acceptor site r

• The specific functions of ERs and AR underline their crucial

  2024-03-30

  

  The specific functions of ERs and AR underline their crucial roles during different phases of spermatogenesis. Their deregulation could affect numerous downstream targets, thereby, disrupting spermatogenesis and male fertility. Various studies have shown that estrogen-like chemicals in the environme

• Sixth significant progress has been made during the

  2024-03-30

  

  Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi

• These mutations induce the gene auto activation in

  2024-03-30

  

  These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations

• Within the PARP family TIPARP is most evolutionarily conserv

  2024-03-30

  

  Within the PARP family, TIPARP is most evolutionarily conserved with PARP12 (ARTD12) and PARP13 (ARTD13) [27,28,41]. All three proteins contain at least one RNA-type CCCH zinc finger domain, a poly-ADP-ribose binding WWE domain and a PARP catalytic domain (Fig. 1). PARP13 is catalytically inactive,

• In a recent series of studies from our laboratory to

  2024-03-30

  

  In a recent series of studies from our laboratory, to characterize the contractile systems within the rat Epibrassinolide wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist induc

• Implicit in this concept is the idea that

  2024-03-30

  

  Implicit in this concept is the idea that the β-adrenoceptors in the detrusor would be activated by adrenergic nerves of the sympathetic system: sympathetic activity promoting relaxation and enhancing bladder capacity. However, it has been demonstrated that there is only a sparse adrenergic innervat

• Whether similar mechanisms play a role in

  2024-03-30

  

  Whether similar mechanisms play a role in adiponectin signal transduction and whether additional proteins are recruited to adiponectin receptors via APPL1 has not been analysed so far. Although it has been clearly established that APPL1 is a downstream adaptor protein in adiponectin signal transduct

• In the presence of detrimental conditions such as inflammati

  2024-03-30

  

  In the presence of detrimental conditions, such as inflammation, hypoxia, ischemia trauma or neoplastic milieu, the extracellular levels of adenosine increase massively, reaching micromolar range [51,52]. In these pathological contexts, adenosine accumulation stems from increased extracellular depho

• BMS-626529 Our initial approach to identify hits was two pro

  2024-03-30

  

  Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI BMS-626529 library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was

• In our previous report we synthesized

  2024-03-29

  

  In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t

• V ATPase is a complex

  2024-03-29

  

  V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial Agarose GPG/LMP low melt of rats has been reported to contain V-ATPase which is distributed at the apical pole of the

• tak1 inhibitor A contribution of V ATPase subunits specifica

  2024-03-29

  

  A contribution of V-ATPase subunits specifically to phagosome-lysosome fusion was uncovered by Peri and Nüsslein-Volhard who described that depletion of the VO subunit a1 in zebrafish interferes with phagosome maturation in microglial tak1 inhibitor (Peri and Nusslein-Volhard, 2008). However, loss

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