• Recently two distinct small molecule inhibitors of PHGDH

  2024-05-25

  

  Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer homoharringtonine with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces th

• br Depletion of serum amino acids Currently the

  2024-05-25

  

  Depletion of serum amino acids Currently, the only anticancer agents that directly target amino AG 1879 metabolism are bacterial l-asparaginases (from Escherichia coli and Erwinia chrysanthemi), which are FDA-approved for treatment of pediatric and adult ALL. A potential complication of using ba

• Lorlatinib is an orally active brain penetrant cyclic aminop

  2024-05-25

  

  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

• TRAM 39 While the mechanisms by which ALDH regulates

  2024-05-25

  

  While the mechanisms by which ALDH2 regulates cardiac responses to pathological stress remain unclear, the capillary rarefaction found in pressure-overloaded ALDH2 Tg hearts provides potential clues. Loss of capillary density and diminished endothelial function occur in pathological hypertrophy [46]

• Globally the total number of patients included

  2024-05-25

  

  Globally, the total number of patients included in the meta-analysis was 1885, ranging from 40 to 442 patients per study. All eligible studies reported the association between ALDH1 expression and patients' OS [24-26, 3241], whereas nine studies evaluated the relationship between ALDH1 expression an

• The activation of the A BR

  2024-05-24

  

  The activation of the A2BR subtype triggers different intracellular metabolic pathways, often linked to the activation of adenylyl cyclase and increased levels of intracellular cAMP (Lynge et al., 2003, Bernareggi et al., 2015). The nAChR-channel ONO-8711 mediated by the cAMP/PKA pathway was report

• Until now five muscarinic receptor

  2024-05-24

  

  Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l

• estrogen related receptor An alternative to the agonist or a

  2024-05-24

  

  An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the

• br Methods br Results and

  2024-05-24

  

  Methods Results and discussion Conclusions Acknowledgements The authors thank Dr. Francois Alhenc-Gelas (then INSERM U367, Paris, France), who kindly provided the plasmid for truncated soluble recombinant human ACE – WTΔ, Dr. Elena Arablinskaya (Institute of Phtiziopulmonology, Moscow, R

• Regarding androgens it is known that they

  2024-05-24

  

  Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco

• From our in vivo studies and previously

  2024-05-24

  

  From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar

• Our sample is representative of mRCC treated with sunitinib

  2024-05-24

  

  Our sample is representative of mRCC treated with sunitinib. However, the results from CCC setting have limited inference due to small exploratory sample (n = 51). Additionally, the significance of survival differences in CCC according to AXL staining is tangential. Unfortunately, we were unable to

• Congruously our findings of voltage electrode clamping

  2024-05-24

  

  Congruously, our findings of voltage-electrode-clamping assays indicate that hipN851K mutation mediates partial loss of Na+/K+-ATPase pump currents, also confirming our thesis that hipN851K mutation acts as a hypomorph. As demonstrated here by our external electrical stimulation studies and ECG reco

• From an historical perspective ligands for

  2024-05-24

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, G007-LK 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 were ra

• DS2 australia Several alterations have been or can be

  2024-05-24

  

  Several alterations have been or can be associated to the decreased tolerance of steatotic liver to I/R injury. Previous studies demonstrated that upregulation of the mitochondrial uncoupling protein-2 (UP2) is strictly related to the increase of I/R injury in steatotic liver [4]. UPR induction is c

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