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 …

The nuclear receptor superfamily: A structural perspective

ER Weikum, X Liu, EA Ortlund - Protein Science, 2018 - Wiley Online Library
Nuclear receptors (NRs) are a family of transcription factors that regulate numerous
physiological processes such as metabolism, reproduction, inflammation, as well as the …

Sex differences in the hypothalamic–pituitary–adrenal axis' response to stress: an important role for gonadal hormones

AL Heck, RJ Handa - Neuropsychopharmacology, 2019 - nature.com
The hypothalamic–pituitary–adrenal (HPA) axis, a neuroendocrine network that controls
hormonal responses to internal and external challenges in an organism's environment …

[HTML][HTML] Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment

HK Patel, T Bihani - Pharmacology & therapeutics, 2018 - Elsevier
Breast cancer is the most frequently diagnosed cancer in women, with estrogen receptor
positive (ER+) breast cancer making up approximately 75% of all breast cancers diagnosed …

Mechanisms mediating the regulation of peroxisomal fatty acid beta-oxidation by PPARα

M Tahri-Joutey, P Andreoletti, S Surapureddi… - International journal of …, 2021 - mdpi.com
In mammalian cells, two cellular organelles, mitochondria and peroxisomes, share the ability
to degrade fatty acid chains. Although each organelle harbors its own fatty acid β-oxidation …

Oral selective estrogen receptor degraders (SERDs) as a novel breast cancer therapy: present and future from a clinical perspective

C Hernando, B Ortega-Morillo, M Tapia… - International journal of …, 2021 - mdpi.com
Estrogen receptor-positive (ER+) is the most common subtype of breast cancer. Endocrine
therapy is the fundamental treatment against this entity, by directly or indirectly modifying …

[HTML][HTML] FXR in liver physiology: Multiple faces to regulate liver metabolism

K Panzitt, M Wagner - Biochimica et Biophysica Acta (BBA)-Molecular Basis …, 2021 - Elsevier
The liver is the central metabolic hub which coordinates nutritional inputs and metabolic
outputs. Food intake releases bile acids which can be sensed by the bile acid receptor FXR …

International union of basic and clinical pharmacology CXIII: Nuclear receptor superfamily—Update 2023

TP Burris, IMS de Vera, I Cote, CA Flaveny… - Pharmacological …, 2023 - Elsevier
The NR superfamily comprises 48 transcription factors in humans that control a plethora of
gene network programs involved in a wide range of physiologic processes. This review will …

Endocrine disrupting chemicals: Impact on human health, wildlife and the environment

T Encarnação, AACC Pais, MG Campos… - Science …, 2019 - journals.sagepub.com
Endocrine disrupting chemicals are a group of pollutants that can affect the endocrine
system and lead to diseases and dysfunctions across the lifespan of organisms. They are …

The orphan nuclear receptors steroidogenic factor-1 and liver receptor homolog-1: structure, regulation, and essential roles in mammalian reproduction

MC Meinsohn, OE Smith, K Bertolin… - Physiological …, 2019 - journals.physiology.org
Nuclear receptors are intracellular proteins that act as transcription factors. Proteins with
classic nuclear receptor domain structure lacking identified signaling ligands are designated …