activator lyn 1604  (MedChemExpress)

Journal: Endocrinology

Article Title: mTOR Regulates Mineralocorticoid Receptor Transcriptional Activity by ULK1-Dependent and -Independent Mechanisms

doi: 10.1210/endocr/bqae015

Figure Lengend Snippet: Primary antibodies with RRID number

Article Snippet: The mTOR activator MHY1435 and its inhibitors AZD-8055, MK-8669, Rapamycin, CC-223, Oxa-01, the ULK1 activator LYN-1604, and its inhibitor MRT-68921 were obtained from Cayman Chemical Company.

Techniques:

Journal: Endocrinology

Article Title: mTOR Regulates Mineralocorticoid Receptor Transcriptional Activity by ULK1-Dependent and -Independent Mechanisms

doi: 10.1210/endocr/bqae015

Figure Lengend Snippet: ULK1 activity in M1-rMR-TAT3-Gluc cells. A, Western blot analysis for the dose-dependent effect of the mTOR inhibitor AZD on ULK1 phosphorylation levels. B, Dose-dependent effect of the ULK1 inhibitor MRT-68921, and C, ULK1 activator LYN-1604 on Aldo-induced MR transactivation. Results are shown as mean ± SEM (n = 3-8). *P < .05 and **P < .01 vs control. Aldo, aldosterone; Cont, control.

Article Snippet: The mTOR activator MHY1435 and its inhibitors AZD-8055, MK-8669, Rapamycin, CC-223, Oxa-01, the ULK1 activator LYN-1604, and its inhibitor MRT-68921 were obtained from Cayman Chemical Company.

Techniques: Activity Assay, Western Blot, Phospho-proteomics, Control

Journal: Endocrinology

Article Title: mTOR Regulates Mineralocorticoid Receptor Transcriptional Activity by ULK1-Dependent and -Independent Mechanisms

doi: 10.1210/endocr/bqae015

Figure Lengend Snippet: Effect of ULK1 or mTOR inhibition on aldo-induced transactivation of MR-S843A in M1-rMR-S843A-TAT3-Gluc cells. A, Introduction of rMR-S843A in M1-TAT3-Gluc cells was confirmed by Western blot. Dose effects of B, MRT-68921, and C, AZD on Aldo stimulation of MR-S843A. Results are shown as mean ± SEM (n = 8). **P < .01 vs control.

Article Snippet: The mTOR activator MHY1435 and its inhibitors AZD-8055, MK-8669, Rapamycin, CC-223, Oxa-01, the ULK1 activator LYN-1604, and its inhibitor MRT-68921 were obtained from Cayman Chemical Company.

Techniques: Inhibition, Western Blot, Control

Journal: Endocrinology

Article Title: mTOR Regulates Mineralocorticoid Receptor Transcriptional Activity by ULK1-Dependent and -Independent Mechanisms

doi: 10.1210/endocr/bqae015

Figure Lengend Snippet: Schematic of possible interactions of the MR, ULK1, and mTOR in M1-rMR-TAT3-Gluc cells. Of several potential and known phosphorylation sites on the MR, only S843 in the ligand binding domain is depicted. A, Basal: physiological ligands activate MR, resulting in dose-responsive increases in MR transcription in response to ligand. Compared to basal: B, ULK1 inhibition decreases S843 phosphorylation, thus number or inactivated MR, and increases MR transcriptional activity in response to ligand. Not shown: No significant effect was observed with ULK1 agonist. C, mTOR inhibition decreases ULK1 inactivation, resulting in an increase in S843 phosphorylation, thus inactivation of the MR and decreased transcription in response to ligand. Not shown: No significant effect was observed with an mTOR agonist. D, The mutation of serine to alanine at position 843 (S843A) does not support phosphorylation, thus preventing ULK1 inactivation of MR, resulting in an increase in MR transcription in response to ligand like that in B. E, mTOR inhibition in cells with the S843A mutation significantly decreased activation of the MR and transcription in response to ligand, but not to the extent as in the cells with wild-type MR in C. MTOR promotes MR activity by an additional mechanism besides ULK1 inhibition.

Article Snippet: The mTOR activator MHY1435 and its inhibitors AZD-8055, MK-8669, Rapamycin, CC-223, Oxa-01, the ULK1 activator LYN-1604, and its inhibitor MRT-68921 were obtained from Cayman Chemical Company.

Techniques: Phospho-proteomics, Ligand Binding Assay, Inhibition, Activity Assay, Mutagenesis, Activation Assay