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br Identification of the kinase that phosphorylates P c
2023-04-07
Identification of the kinase that phosphorylates P450c17 The first Ser/Thr kinase that phosphorylates P450c17 was identified only recently. Of the 518 kinases in the human ‘kinome’ 278 are Ser/Thr kinases (Manning et al., 2002), but microarrays identified only 145 Ser/Thr kinases in human NCI-H29
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br Cytochrome b br Cytochrome
2023-04-07
Cytochrome b5 Cytochrome P450 17α-hydroxylase/17,20-lyase (P450 17A1) A number of P450s involved in steroid biosynthesis are multifunctional as they carry out two or more sequential hydroxylation reactions on the same substrate(s). P450 17A1 is a dual function endoplasmic reticulum enzyme enco
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Here we show that the co activation of RTKs
2023-04-07
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC TC-I 15 mg and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-000
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Introduction The MMR system keeps the fidelity of replicatio
2023-04-07
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
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br The role of LOX
2023-04-06
The role of 12/15-LOX plays in autophagy Autophagy is a process by which cellular material is delivered to lysosomal to degrade the damaged organelles and proteins to facilitate nutrient recycling (Towers and Thorburn, 2016). There has been characterized three types of autophagy-macroautophagy, m
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The importance of the ATM Tel to ATR
2023-04-06
The importance of the ATM/Tel1 to ATR/Mec1 switch in the response to DSBs remains to be determined. Noteworthy, resection-defective S. cerevisiae cells, such as sae2Δ, exo1Δ, fun30Δ or sgs1Δ mutants, fail to turn off the checkpoint in response to an unrepaired DSB [56], [127], [128]. Moreover, the s
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SU 4312 At the outset of targeting the two Gln side
2023-04-06
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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The structural analysis of the ASK activation segment which
2023-04-06
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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br Discussion br Acknowledgments Writing
2023-04-06
Discussion Acknowledgments Writing of this review and collection of data from our laboratories that are presented were supported by a grant from the Belgian Science Policy (BELSPO) SSTC Interuniversity Attraction Poles Plastoscine P7/17 to AVDL and JB, multiple grants from the Fund for Scienti
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br Introduction Rhamdia quelen jundi Silurifomes Heptapterid
2023-04-06
Introduction Rhamdia quelen (jundiá, Silurifomes, Heptapteridae) is a neotropical catfish widely distributed in Central and South America (Silfvergrip, 1996). This species shows high potential for the aquaculture industry, due to an elevated growth rate, good carcass yield, and easy reproduction
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Mitochondria are key organelles involved
2023-04-06
Mitochondria are key organelles involved in the mechanism of apoptosis (Xiong et al., 2014), and loss of ΔΨm is an important marker associated with mitochondrial dysfunction and cell death. We found that Mino induced ΔΨm impairment and nuclear fragmentation in Jurkat calcium channel in a concentrati
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Under some pathological conditions AT R internalization
2023-04-06
Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v
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Numerous studies have shown that
2023-04-06
Numerous studies have shown that ω-3 PUFA incorporation into the lipid raft can affect the distribution and function of protein in the lipid raft by altering raft composition [25], [26], [27]. For example, DHA treatment excluded phospholipase D (PLD) from lipid raft toward non-lipid raft, resulting
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We investigated the role of ABT treatment in
2023-04-06
We investigated the role of ABT 702 treatment in MAPKinase activation in mouse microglia in vitro. In Fig. 7D immunocytochemistry results revealed that Iba1 and p-ERK1/2 co-localized in LPS induced mouse microglia. In our previous study we have reported that LPS activates ERK1/2 phosphorylation (Ahm
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A high throughput small molecule ACK biochemical inhibition
2023-04-06
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Irinotecan to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was p
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