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In conclusion we designed novel E inhibitors based on the
2021-08-16

In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and , we f
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Plasminogen is composed of five N terminal kringle
2021-08-16

Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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In contrast to SQLE HMGCR could be efficiently degraded
2021-08-16

In contrast to SQLE, HMGCR could be efficiently degraded in YM 58483 sale lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our rece
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In most cases patients will not present immediately after
2021-08-16

In most cases, patients will not present immediately after SM exposure because SM-induced clinical symptoms typically occur after a latency period of several hours [8], [9], [10]. When they do present, the detection of free, unbound alkylating agent is highly unlikely. For this reason, available rap
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What does this mean for cancer therapy
2021-08-16

What does this mean for cancer therapy? We found that components of the de novo pyrimidine synthesis pathway rarely mutate in cancer, clearly showing its importance. In our experimental models, the pathway, including DHODH itself, was primed to respond when the block in CoQ redox-cycling was removed
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MTX and MTXPGs block the activity of the
2021-08-16

MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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CYP enzymes have an important role in microsomal oxidase
2021-08-14

CYP450 Chlorogenic acid have an important role in microsomal oxidase function across a broad range of taxa (Pakharukova et al., 2012). They are involved in metabolism and detoxification of both internally generated compounds and xenobiotics as the phase I metabolizing enzymes and play an important r
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Today many strategies have been developed to enhance CXCR
2021-08-14

Today, many strategies have been developed to enhance CXCR-4 receptor Gossypol on the cell surface, either by modifying the cell culture medium or by modifying the CXCR-4 gene in BMSCs to stimulate stem cell recruitment (Jiang et al., 2012, Liu et al., 2014b). For instance, the pre-conditioning of
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The large body of structural knowledge
2021-08-14

The large body of structural knowledge that is currently available for CRM1 has contributed to atomic level and mechanistic understanding of many steps in the CRM1 nuclear export cycle. However, structural analysis could still inform on several outstanding questions and guide future discoveries pert
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Fear like behaviors are produced by intracerebroventricular
2021-08-14

Fear-like behaviors are produced by intracerebroventricular CRF administration (Meloni et al., 2006, Radulovic et al., 1999), as well its administration into specific cytidine areas such as the amygdala (Daniels et al., 2004, Donatti and Leite-Panissi, 2011), the periaqueductal gray matter (Martins
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br Conclusion In this review we have discussed how inhibitio
2021-08-14

Conclusion In this review, we have discussed how inhibition of the CK2/CDK5 signaling axis protects WM only when inhibited before ischemia, while inhibition of the CK2/AKT/GSK3β signaling axis protects WM either before or after an ischemic injury in young, aging, and old WM (Fig. 3). CK2 activati
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Edrophonium chloride receptor In S cerevisiae Mek a paralog
2021-08-14

In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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EP is the major receptor to mediate PGE induced inflammatory
2021-08-14

EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by angiotensin receptor blockers in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3],
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It has been reported that PGE increases expression of
2021-08-14

It has been reported that PGE2 increases expression of the survivin mRNA (Baratelli et al. 2005) and promotes the stabilization of the survivin protein in some tumor 51 8 (Krysan et al. 2003). However, it is unclear whether PGE2 affects the expression of survivin mRNA or promotes the stabilization o
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br Materials and methods br Results br Discussion
2021-08-14

Materials and methods Results Discussion Enolase (2-phospho-D-glycerate hydrolase) is a glycolytic enzyme that is also involved with various important roles in the intracellular and extracellular space (Copley, 2003; S. Zhang et al., 2015) such as transcriptional regulation, apoptosis, grow
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