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To study the effect of DDR
2021-08-19
To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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ER redox imbalance leads to the
2021-08-19
ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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Given the link between E s autoimmunity and
2021-08-19
Given the link between E3s, autoimmunity, and antitumor immunity, it nrf2 inhibitor is reasonable to assume that, similar to other ICBs, IRAEs may limit the clinical use of E3-targeting therapies – further stressing the need to better understand the underlying mechanisms of these unwanted effects. D
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motilin receptor br Materials and methods br
2021-08-19
Materials and methods Results Discussion Tuberculosis is caused by the mycobacterium M. tuberculosis, a pathogen able to survive in the hostile conditions through sophisticated defence mechanisms. In an attempt to clarify some aspects of the M. tuberculosis defence mechanisms, we have inves
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The unique property of mutant IDH
2021-08-19
The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pre
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br Conflict of interest br Acknowledgements This work was fu
2021-08-19
Conflict of interest Acknowledgements This work was funded by the National Science Centre, Poland, grant number N N303 571539. We are greatly indebted to Patrick Fox for help with the final manuscript. Introduction Alkylating agents which interact directly with DNA to form covalent bonds h
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br Molecular modeling study Molecular modeling study was
2021-08-19
Molecular modeling study Molecular modeling study was essentially needed to understand and interpret the DHFR inhibitory pattern of this new class of compounds. Computational docking is an algorithm designed to estimate two main terms. The first is to determine the suitable position and the orien
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There is literature precedence for the metabolic
2021-08-19
There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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In anticipation of an approach based on modification of the
2021-08-19
In anticipation of an approach based on modification of the cyclohexylacetic ro3 subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1, although they
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We had earlier reported that
2021-08-19
We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen
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d-amphetamine mg The in vitro enantioselective metabolism of
2021-08-19
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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ARCA An increased CK activity was found
2021-08-18
An increased CK2 activity was found in septal neuronal ARCA dissected from rat embryos after hypoglycemia [36]. These data indicated that CK2 activity is not only regulated by insulin but also by the glucose concentration. One essential step in insulin action is the binding of the hormone to speci
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T helper Th cells play a central role
2021-08-18
T helper (Th) TDZD-8 play a central role in activation of immune system against infectious agents through secretion of lymphokines or cytokines. African trypanosomes target the Th cells and alter their activation, possibly for their own survival and perpetuity (Namangala, 2011). Trypanosoma brucei
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Our earlier experimental studies showed neutral i e non
2021-08-18
Our earlier experimental studies showed "neutral", i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]]. The next step was to investigate whether thi
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br Discussion Variable estradiol effects on
2021-08-18
Discussion Variable estradiol effects on cell proliferation have been reported according to animal species, tissues, and type of estrogen receptor [16,21,22,[29], [30], [31]]. In the kidney, 17βE was found to increase [3H]-thymidine incorporation in primary rabbit kidney proximal tubule Temozolom
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