• On the basis of the above

  2023-11-20

  

  On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote

• The difficulty of characterizing nAChRs in the central

  2023-11-20

  

  The difficulty of characterizing nAChRs in the central nervous system is also exemplified by early observations that nicotine caused no detectable effect when applied on a brain slice and it is only with the focal and high time resolution of more recent experiments that the effects of nicotinic neur

• Aminoglutethimide first generation aromatase inhibitor has b

  2023-11-20

  

  Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome

• According to the present observations the Ampk isoform promo

  2023-11-20

  

  According to the present observations, the Ampkα1 isoform promotes AP-1 transcriptional activity and thereby fosters 20(S)-Hydroxycholesterol of AP-1 target genes in cardiomyocytes via activation of Pkcζ. The transcription factor AP-1 plays a decisive role during cardiac remodeling [24], [25], [26],

• Pathological angiogenesis occurs when an imbalance of endoge

  2023-11-20

  

  Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance

• The increased occurrence of ARIA E in APOE carriers in

  2023-11-20

  

  The increased occurrence of ARIA-E in APOE ε4 carriers in phase 2 studies resulted in separate protocols for carriers and noncarriers in the subsequent phase 3 studies. Two 18-month trials comprising 1121 carriers and 1331 noncarriers with mild to moderate AD tested doses of bapineuzumab that varied

• br Animal models of NAFLD Human research has

  2023-11-18

  

  Animal models of NAFLD Human research has greatly shaped our understanding of non-alcoholic fatty liver disease, but several limitations exist in studying the disease processes in humans, such as variations in environmental exposure, pre-existing genetic risk factors, racial and ethnic difference

• Lorlatinib is an orally active brain penetrant cyclic aminop

  2023-11-18

  

  Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F

• We found evidence of the interaction between

  2023-11-18

  

  We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th

• It thus appeared reasonable that AR needed to

  2023-11-18

  

  It thus appeared reasonable that AR needed to be inhibited and great experimental efforts began which are still on-going [6]. Indeed, hundreds of ARIs have been characterized but no significant drug development has followed. The case of Sorbinil, which did not pass clinical trials is emblematic [7]

• Within the PARP family TIPARP is most evolutionarily conserv

  2023-11-18

  

  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,

• AdipoRon is an orally active

  2023-11-18

  

  AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r

• A high throughput screening campaign led

  2023-11-18

  

  A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity

• Consistent with the above prediction there are additional re

  2023-11-17

  

  Consistent with the above prediction, there are additional reports in which HMGA proteins have been demonstrated to facilitate recruitment of chromatin remodeling complexes to gene regulatory regions containing positioned nucleosomes during the transcriptional activation process. One particularly il

• br Methodology br Antibiotics in lakes br Antibiotic

  2023-11-17

  

  Methodology Antibiotics in lakes Antibiotic resistance genes in lakes Perspectives of study on ProteOrange and ARGs in lakes Conclusion This paper systematically reviewed the distribution of antibiotics and ARGs in global lakes. A total of 57 antibiotics reported at least once in the

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