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Consistent with the observation that mutations in
2023-10-27

Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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Aurora B is also very important in
2023-10-27

Aurora-B is also very important in proper cytokinesis. In the absence of Aurora-B mediated phosphorylation of Ser72 in vimentin, the two daughter cells remain attached to each other through bridges of cytoplasm; cytokinesis fails [31]. Other Aurora-B dependent proteins that are important for cytokin
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Here we report discovery of highly selective
2023-10-27

Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of BPTES bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To iden
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These results must also be addressed in
2023-10-27

These results must also be addressed in light of porcine AMPKγ3R200Q (RN−) mutation. Pigs harboring this mutation produce meat with an abnormally low ultimate pH (pHas TW-37 meat (Copenhafer et al., 2006, Lundström et al., 1998, Milan et al., 2000). This extremely low pH is very close to the isoele
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Comparison of the GLUT positive
2023-10-27

Comparison of the GLUT1-positive plus ACLY negative group with the GLUT1-negative plus ACLY positive group indicated no significant difference with respect to disease-free survival and overall survival. However, some obvious differences in histological types were found in their formation. A previous
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In Rainey et al published the results
2023-10-27

In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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br Funding This study was supported
2023-10-27

Funding This study was supported by Grant UM1-CA186690 (NCI-CTEP) and R01CA204173 (CJB). This project used the UPCI Cancer Pharmacokinetics and Pharmacodynamics Facility (CPPF) and was supported in part by award P30-CA47904 and R50CA211241. Introduction Despite the efficacy of platinum based
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Pravastatin sodium The compounds containing beryllium act as
2023-10-27

The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be Pravastatin sodium []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely strong bide
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Apelin is a bioactive peptide and endogenous
2023-10-26

Apelin is a bioactive peptide and endogenous ligand for the APJ receptor (APLNR), a member of the G protein coupled receptor family that shares a similar sequence as the angiotensin type-1 receptor (AT1) [5]. Early studies demonstrated that the apelin/APLNR receptor axis plays a significant role in
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In past Zebra fish Danio rerio has
2023-10-26

In past, Zebra fish (Danio rerio) has emerged as a suitable model for early vertebrate development, and a number of targeted mutations in the zebrafish genome led to phenotypic alterations that resemble human diseases [34]. A 12-LOX in Zebra fish has been cloned and knock down of this zf12-LOX enzym
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AMG 9810 receptor It has been largely demonstrated that seve
2023-10-26

It has been largely demonstrated that several clinico-pathological factors influence ovarian cancer patients' prognosis, including residual tumor at primary cytoreductive surgery, FIGO stage, tumor grading, cancer histology and performance status [3,4]. Nevertheless, the recent awareness achieved in
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br Conclusion Biotransformation of trachyloban oic
2023-10-26

Conclusion Biotransformation of trachyloban-19-oic Gastrodin by S. racemosum provided three products. Oxidation of compound 1 at C-17 (2–3), as well as rearrangement of 1 into a kaurane diterpene hydroxylated in C-16 and C-17 (4) were crucial for increasing AChE inhibitory activity. Compound 3 w
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An alternative to the agonist or antagonist potential in
2023-10-26

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
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The difficulty of characterizing nAChRs in the central
2023-10-26

The difficulty of characterizing nAChRs in the central nervous system is also exemplified by early observations that nicotine caused no detectable effect when applied on a brain slice and it is only with the focal and high time resolution of more recent experiments that the effects of nicotinic neur
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The structure of LO is
2023-10-26

The structure of 5-LO is divided in two domains, the catalytic C-terminal domain and the N-terminal regulatory C2-like domain (C2ld) [59,60]. The C2ld spans the GSK3787 1-114 and is responsible for translocation and binding of calcium and membranes [61–63]. The catalytic domain is primarily an α-hel
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