• Accessibility and physico chemical features of

  2022-06-22

  

  Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom

• Glycogen synthase kinase GSK is an evolutionarily conserved

  2022-06-22

  

  Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy

• Continuing studies of endocannabinoid ligands at GPR reveal

  2022-06-21

  

  Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort

• 11-dUTP br Author contributions br Acknowledgements

  2022-06-21

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

• Transporters are important ta http www apexbt com

  2022-06-21

  

  Transporters are important targets for devising new therapies, optimizing existing therapies, and helping understand the toxicities of certain drugs. Given the well-documented role of transporters in restricting the distribution of drugs, modulating the relevant transporters could enhance the permea

• Inhibitors against the proteasome a component

  2022-06-21

  

  Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor RI-1 and were shown to induce apoptos

• Of note the intracellular egg compartment exhibiting SA gal

  2022-06-21

  

  Of note, the intracellular egg compartment exhibiting SA-β-gal activity also exhibits lipofuscin auto-fluorescence (Fig. 6B), and it is co-stained with the lipid-specific dye SBB (Supplemental Fig. 5). On the one hand, these findings reflect the fact that the pool of yolk protein contains lipoprotei

• Corresponding to the different insulinotropic signaling the

  2022-06-21

  

  Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Autophagy Compound Library on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site

• To meet the requirement of ferroptosis based therapy a

  2022-06-21

  

  To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous

• One of the main mechanisms

  2022-06-21

  

  One of the main mechanisms enabling recycling of intracellular redox-active iron is lysosomal degradation of ferritin in the process of autophagy, often referred to as ‘ferritinophagy’ [128]. Autophagy was suggested to contribute to ferroptotic cell death by promoting the degradation of iron storage

• During the activation of the coagulation cascade factor

  2022-06-21

  

  During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium VX-702 on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit platele

• luteolin Following the discovery of diketo compounds

  2022-06-20

  

  Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent luteolin based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioas

• Dithiodipyridine also known as aldrithiol is a known zinc

  2022-06-20

  

  2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency Deferiprone australia type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamine di

• br Histamine and glycaemia Histamine is

  2022-06-20

  

  Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of put you down and diabetes date back to the 1950s. Since that time the involvement of histamine in d

• Anti apoptotic Bcl proteins have become attractive targets f

  2022-06-20

  

  Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w

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