Results 1 to 10 of about 734,603 (316)

Carboxylic Acid Bioisosteres in Medicinal Chemistry: Synthesis and Properties

open access: yesJournal of Chemistry, 2022
Lead optimization represents the tedious process of fine-tuning lead compounds from biologically active hits to suitable drug candidates for clinical trials.
Kato Bredael   +4 more
doaj   +1 more source

How the glucocorticoid receptor contributes to platinum-based therapy resistance in solid cancer

open access: yesNature Communications, 2021
Synthetic glucocorticoids serve as co-medication against solid malignant tumors. However, glucocorticoid receptor activation may promote unsolicited cancer resistance to chemotherapy.
Dorien Clarisse, Karolien De Bosscher
doaj   +1 more source

Meta‐analysis and Consolidation of Farnesoid X Receptor Chromatin Immunoprecipitation Sequencing Data Across Different Species and Conditions

open access: yesHepatology Communications, 2021
Farnesoid X receptor (FXR) is a nuclear receptor that controls gene regulation of different metabolic pathways and represents an upcoming drug target for various liver diseases.
Emilian Jungwirth   +4 more
doaj   +1 more source

Selective PPARα Modulator Pemafibrate and Sodium-Glucose Cotransporter 2 Inhibitor Tofogliflozin Combination Treatment Improved Histopathology in Experimental Mice Model of Non-Alcoholic Steatohepatitis

open access: yesCells, 2022
Ballooning degeneration of hepatocytes is a major distinguishing histological feature of non-alcoholic steatosis (NASH) progression that can lead to cirrhosis and hepatocellular carcinoma (HCC).
Kentaro Murakami   +14 more
doaj   +1 more source

Transcriptional repression shapes the identity and function of tissue macrophages

open access: yesFEBS Open Bio, 2021
The changing extra‐ and intracellular microenvironment calls for rapid cell fate decisions that are precisely and primarily regulated at the transcriptional level.
Krisztian Bene   +2 more
doaj   +1 more source

Compound A influences gene regulation of the Dexamethasone-activated glucocorticoid receptor by alternative cofactor recruitment

open access: yesScientific Reports, 2017
The glucocorticoid receptor (GR) is a transcription factor of which the underlying gene regulatory mechanisms are complex and incompletely understood. The non-steroidal anti-inflammatory Compound A (CpdA), a selective GR modulating compound in various ...
S. J. Desmet   +9 more
doaj   +1 more source

Improved Glucocorticoid Receptor Ligands: Fantastic Beasts, but How to Find Them?

open access: yesFrontiers in Endocrinology, 2020
Exogenous glucocorticoids are widely used in the clinic for the treatment of inflammatory disorders and hematological cancers. Unfortunately, their use is associated with debilitating side effects, including hyperglycemia, osteoporosis, mood swings, and ...
Laura Van Moortel   +7 more
doaj   +1 more source

Mechanisms Underlying the Functional Cooperation Between PPARα and GRα to Attenuate Inflammatory Responses

open access: yesFrontiers in Immunology, 2019
Glucocorticoids (GCs) act via the glucocorticoid receptor (NR3C1, GRα) to combat overshooting responses to infectious stimuli, including lipopolysaccharide (LPS).
Nadia Bougarne   +24 more
doaj   +1 more source

Transcriptional Profiling of Monocytes Deficient in Nuclear Orphan Receptors NR4A2 and NR4A3 Reveals Distinct Signalling Roles Related to Antigen Presentation and Viral Response

open access: yesFrontiers in Immunology, 2021
The nuclear receptor sub-family 4 group A (NR4A) family are early response genes that encode proteins that are activated in several tissues/cells in response to a variety of stressors.
David E. Phelan   +13 more
doaj   +1 more source

Comprehensive and systemic optimization for improving the yield of SARS-CoV-2 spike pseudotyped virus

open access: yesMolecular Therapy: Methods & Clinical Development, 2021
Virus neutralization assay is principally conducted by measuring the ability of the antibodies in patient sera to prevent the infection of susceptible cells by the virus.
Xinping Fu, Lihua Tao, Xiaoliu Zhang
doaj  

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