Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm00336a003 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer.
Br J Cancer
July 2023
Swansea University Medical School, Swansea University, Swansea, SA2 8PP, UK.
Background: Epigenomic dysregulation has been linked to solid tumour malignancies, including ovarian cancers. Profiling of re-programmed enhancer locations associated with disease has the potential to improve stratification and thus therapeutic choices. Ovarian cancers are subdivided into histological subtypes that have significant molecular and clinical differences, with high-grade serous carcinoma representing the most common and aggressive subtype.
View Article and Find Full Text PDFBupivacaine Metabolite Can Interfere with Norfentanyl Measurement by LC-MS/MS.
J Appl Lab Med
June 2022
Department of Pathology, Massachusetts General Hospital and Harvard Medical School, Boston, MA.
Background: Liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) is the gold standard for the measurement of fentanyl and norfentanyl (NF) in urine and is favored over immunoassays due to its superior specificity. NF is the principal metabolite of fentanyl found in the urine and is typically present in higher abundance than fentanyl. Thus, the sensitivity and specificity of LC-MS/MS relies largely on the ability to identify and quantitate NF.
View Article and Find Full Text PDFML277 regulates KCNQ1 single-channel amplitudes and kinetics, modified by voltage sensor state.
J Gen Physiol
December 2021
Department of Anesthesiology, Pharmacology and Therapeutics, University of British Columbia, Vancouver, Canada.
KCNQ1 is a pore-forming K+ channel subunit critically important to cardiac repolarization at high heart rates. (2R)-N-[4-(4-methoxyphenyl)-2-thiazolyl]-1-[(4-methylphenyl)sulfonyl]-2 piperidinecarboxamide, or ML277, is an activator of this channel that rescues function of pathophysiologically important mutant channel complexes in human induced pluripotent stem cell-derived cardiomyocytes, and that therefore may have therapeutic potential. Here we extend our understanding of ML277 actions through cell-attached single-channel recordings of wild-type and mutant KCNQ1 channels with voltage sensor domains fixed in resting, intermediate, and activated states.
View Article and Find Full Text PDFPharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
Nat Chem Biol
February 2018
Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts, USA.
Cyclin-dependent kinase 9 (CDK9), an important regulator of transcriptional elongation, is a promising target for cancer therapy, particularly for cancers driven by transcriptional dysregulation. We characterized NVP-2, a selective ATP-competitive CDK9 inhibitor, and THAL-SNS-032, a selective CDK9 degrader consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). To our surprise, THAL-SNS-032 induced rapid degradation of CDK9 without affecting the levels of other SNS-032 targets.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!