• Several dehidropregnenolone derivatives functionalized at C

  2023-09-21

  

  Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic

• br Results and discussion br Conclusion

  2023-09-21

  

  Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen Spironolactone s

• hippo signaling pathway The activity of an enzyme may be reg

  2023-09-21

  

  The activity of an enzyme may be regulated allosterically as well as transcriptionally. We have consistently studied REMS deprivation (REMSD) associated NA mediated allosteric regulation of Na-K ATPase activity in neurons and glia in vivo and in vitro (Amar and Mallick, 2015; Amar et al., 2016; Bask

• Introduction The MMR system keeps the

  2023-09-21

  

  Introduction The MMR system keeps the fidelity of replication by repairing replication errors such as base-base mispairs and insertions/deletions. It plays a substantial role in restoring the fidelity of DNA and contributing to genome integrity [1]. The components of MMR are conserved in a broad ra

• crizotinib Introduction Hepatocellular carcinoma HCC is one

  2023-09-21

  

  Introduction Hepatocellular carcinoma (HCC) is one of the most difficult cancers to treat, and it threatens human health severely [1]. Although various interventions, including surgical operation, radiofrequency ablation, and chemotherapy, have been endorsed, the prognosis of HCC patients remains p

• AT signaling is distinct to that of AT Kaschina

  2023-09-21

  

  AT2 signaling is distinct to that of AT1 (Kaschina and Unger, 2003). As shown here, opposite to the stimulating effect of AT1 signaling, it inhibits apelin secretion. Activation of AT2 receptor, which is also G-protein coupled, is known to decrease cAMP and cGMP levels by inhibiting adenylyl cyclase

• It has been proven that genetic polymorphisms

  2023-09-21

  

  It has been proven that genetic polymorphisms can play an important role in development of hypertension and CVDs. In a Turkish population-based study, it was found that the APLNR gene (rs948847-A445C) polymorphism was not associated with coronary artery disease (CAD), but it was shown to be related

• ALW-II-41-27 receptor br Materials and method br Results br

  2023-09-21

  

  Materials and method Results Discussion Although several studies have showed the crude extracts of K. senegalensis possessed the anti-inflammatory and hypertensive activities (Olayinka et al., 1992). However, the anti-inflammatory effect and underlying molecular mechanisms of its bioactive

• br Small molecule homoisoflavonoid in combination with anti

  2023-09-21

  

  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

• Adenosine is a ubiquitous homeostatic substance

  2023-09-20

  

  Adenosine is a ubiquitous homeostatic substance released from most cells, including neurons and glias. Endogenous adenosine acts at four principal G-protein-associated receptor subtypes: A1, A2a, A2b and A3 (Ralevic and Burnstock, 1998). The stimulation of adenosine receptors by extracellular adenos

• Introduction Mammalian cells express the seven

  2023-09-20

  

  Introduction Mammalian bupropion hydrochloride receptor express the seven STAT family members STAT1, −2, −3, −4, −5A, −5B, and −6 [1], [2]. All STATs exert physiologically important roles as homo- and heterodimers [2], [3], [4]. Cytokines and growth factors activate STATs through the activation of

• Steroidal CYP inhibitors can further be classified

  2023-09-20

  

  Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a

• Phospholipases cleave membrane phospholipids from inflammato

  2023-09-20

  

  Phospholipases cleave membrane phospholipids from inflammatory cells, activated platelets, erythrocytes, adipocytes and cancer Bestatin receptor (Aoki et al., 2008, Neidlinger et al., 2006). Several reports have analysed the role of LPA and its receptors in the pathogenesis of RA. Zhao et al. repo

• br Expression of autotaxin in cancer Autotaxin

  2023-09-20

  

  Expression of autotaxin in cancer Autotaxin (ATX) is a member of the family of NPPs (Nucleotides pyrophosphatases phosphodiesterases (NPP) family with a unique lysophospholipase D (lysoPLD) activity, allowing the synthesis of LPA from lysophospholipid precursors such as the lysophosphatidylcholin

• To identify the kinase s mediating H S phosphorylation

  2023-09-20

  

  To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with Raltitrexed specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck) containing 194

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