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A rational approach for the design of new steroid compounds
2025-02-20
A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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Consistent with the observation that mutations in the redox
2025-02-20
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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Ryoichi et al modified potent clinical candidate VX with
2025-02-20
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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While high fat diet models of insulin resistance are accepta
2025-02-20
While high-fat diet models of insulin resistance are acceptable approaches for the study of pre-diabetes in humans, they are not suitable for modeling progression towards established type2 diabetes. The pattern of activation of the lipoxygenase pathway in pre-clinical models of type2 diabetes has no
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PGC mediated mitochondrial biogenesis in
2025-02-19
PGC-1α-mediated mitochondrial biogenesis in brown fat and endothelial dutp is in part regulated by eNOS and NO [28], [29]. Recent studies indicate that H2S not only augments NO bioavailability and signaling [11], [17], but provides protection against cardiac injury in an eNOS-dependent manner [15],
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Recently rather than predicting categorical variables as in
2025-02-19
Recently, rather than predicting categorical variables as in classification, several studies begin to estimate continuous clinical variables from EP4 signaling inhibitor images. Therefore, instead of classify a subject into binary or multiple pre-determined categories or stages of the disease, regre
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We start with a basic description of
2025-02-19
We start with a basic description of the MT-SGL model. Consider a multi-task learning (MTL) setting with k tasks. Let p be the number of covariates, shared across all the tasks, and n be the number of samples. Let denote the matrix of covariates, be the matrix of responses with each row correspondin
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AR is an enzyme involved in conversion
2025-02-19
AR is an enzyme involved in conversion of glucose into sorbitol using NADPH as a cofactor [46]. This AR polyol pathway generates sorbitol accumulation and NADPH depletion. NADPH participates in detoxification via glutathione (GSH) reductase pathway [47]. Therefore, reduction of NADPH attenuates remo
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br Conflict of interest statement br Introduction Human
2025-02-19
Conflict of interest statement Introduction Human saliva contains many detoxifying and antioxidant L002 like glutathione S-transferase, catalase, peroxidase, aldehyde dehydrogenase (ALDH), etc. [1]. Human salivary ALDH (hsALDH) protects individuals from toxic aldehydes contained in food as nat
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br Downstream signalling of AKT A consensus phosphorylation
2025-02-19
Downstream signalling of AKT A consensus phosphorylation motif has been described for AKT substrates: R-X-R-X-X-S/T-B where X represents any amino apexbio dilution and B represents bulky hydrophobic residues (Alessi, Caudwell, Andjelkovic, Hemmings, & Cohen, 1996). Numerous AKT substrates have b
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br Acknowledgements Dr Paul J
2025-02-19
Acknowledgements Dr. Paul J. Gasser is supported by the National Institutes of Health (grant number R01DA032895), and the Charles E. Kubly Mental Health Research Center. Dr. Christopher A. Lowry is supported by the National Institutes of Health (grant number R21 MH116263), the Department of the N
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As an alternative to chronic receptor
2025-02-19
As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify Imiquimod hydrochloride adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK
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Finally one can ask whether these results throw any light
2025-02-19
Finally, one can ask whether these results throw any light on the nature of the target in SNMG patients. Interestingly, the results of the in vitro incubations suggested that SNMG sera might increase AChR expression to a small extent, raising the possibility that SNMG patients, who have thymic chan
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Until now five muscarinic receptor M
2025-02-18
Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l
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br Dihydrotestosterone in adult fish and frogs br New
2025-02-18
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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