Targeting transcription factors in cancer—from undruggable to reality

JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …

Transcriptional control of energy metabolism by nuclear receptors

C Scholtes, V Giguère - Nature reviews Molecular cell biology, 2022 - nature.com
Transcriptional regulation of catabolic pathways is a central mechanism by which cells
respond to physiological cues to generate the energy required for anabolic pathways …

RORγt protein modifications and IL-17-mediated inflammation

R Kumar, AL Theiss, K Venuprasad - Trends in immunology, 2021 - cell.com
RORγt, the master transcription factor for cytokine interleukin (IL)-17, is expressed explicitly
in Th17 cells, γδT cells, and type 3 innate lymphoid cells in mice and humans. Since …

Progesterone action in endometrial cancer, endometriosis, uterine fibroids, and breast cancer

JJ Kim, T Kurita, SE Bulun - Endocrine reviews, 2013 - academic.oup.com
Progesterone receptor (PR) mediates the actions of the ovarian steroid progesterone, which
together with estradiol regulates gonadotropin secretion, prepares the endometrium for …

Principles for modulation of the nuclear receptor superfamily

H Gronemeyer, JÅ Gustafsson, V Laudet - Nature reviews Drug …, 2004 - nature.com
Nuclear receptors are major targets for drug discovery and have key roles in development
and homeostasis, as well as in many diseases such as obesity, diabetes and cancer. This …

[HTML][HTML] Estrogen receptor-α directs ordered, cyclical, and combinatorial recruitment of cofactors on a natural target promoter

R Métivier, G Penot, MR Hübner, G Reid, H Brand… - Cell, 2003 - cell.com
Transcriptional activation of a gene involves an orchestrated recruitment of components of
the basal transcription machinery and intermediate factors, concomitant with an alteration in …

Cyclical DNA methylation of a transcriptionally active promoter

R Métivier, R Gallais, C Tiffoche, C Le Péron… - Nature, 2008 - nature.com
Processes that regulate gene transcription are directly under the influence of the genome
organization. The epigenome contains additional information that is not brought by DNA …

LXRS and FXR: the yin and yang of cholesterol and fat metabolism

NY Kalaany, DJ Mangelsdorf - Annu. Rev. Physiol., 2006 - annualreviews.org
▪ Abstract Liver X receptors (LXRs) and farnesoid X receptor (FXR) are nuclear receptors
that function as intracellular sensors for sterols and bile acids, respectively. In response to …

Vitamin D and evolution: Pharmacologic implications

A Hanel, C Carlberg - Biochemical pharmacology, 2020 - Elsevier
Vitamin D 3 is produced non-enzymatically when the cholesterol precursor 7-
dehydrocholesterol is exposed to UV-B, ie, evolutionary the first function of the molecule was …

[HTML][HTML] Genomic signaling of vitamin D

C Carlberg - Steroids, 2023 - Elsevier
It took several hundred million years of evolution, in order to develop the endocrine vitamin
D signaling system, which is formed by a nuclear receptor, the transcription factor VDR …