Selective progesterone receptor modulator

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90 YEARS OF PROGESTERONE Progesterone receptor signaling in the normal breast and its implications for cancer

Progesterone is considered as the pregnancy hormone and acts on many different target tissues. Progesterone receptor (PR) signaling is important for normal development and the physiologic function of the breast and impinges on breast carcinogenesis. Both s ...

BIOSCIENTIFICA LTD2020

Targeting the oncogenic signaling of the transcription factor STAT3 with potent and selective monobody inhibitors

Grégory La Sala

Many targeted cancer therapies fail to improve the overall survival of patients. Limitations involve low drug selectivity and the rapid development of resistance. Moreover, the majority of oncogenic drivers presently remain considered as undruggable as th ...

EPFL2020

KAP1 targets actively transcribed genomic loci to exert pleomorphic effects on RNA polymerase II activity

Didier Trono, Evaristo Jose Planet Letschert, Marco Cassano, Annamaria Kauzlaric, Suk Min Jang

KAP1 (KRAB-associated protein 1) is best known as a co-repressor responsible for inducing heterochromatin formation, notably at transposable elements. However, it has also been observed to bind the transcription start site of actively expressed genes. To a ...

2020

The Gene-Regulatory Footprint of Aging Highlights Conserved Central Regulators

Johan Auwerx, Richardus Houtkooper, Maroun Bou Sleiman, Xu Wang, Pooja Jha

Many genes and pathways have been linked to aging, yet our understanding of underlying molecular mechanisms is still lacking. Here, we measure changes in the transcriptome, histone modifications, and DNA methylome in three metabolic tissues of adult and ag ...

2020

New 2-Ethylthio-4-methylaminoquinazoline derivatives inhibiting two subunits of cytochrome bc1 in Mycobacterium tuberculosis

Stewart Cole, Andrej Benjak, Anthony Vocat, Jérémie Piton, Shi-Yan Caroline Foo, Andréanne Lupien

The emergence of multi-drug (MDR-TB) and extensively-drug resistant tuberculosis (XDR-TB) is a major threat to the global management of tuberculosis (TB) worldwide. New chemical entities are of need to treat drug-resistant TB. In this study, the mode of ac ...

2020

Selective hydrogenation of lignin-derived compounds under mild conditions

Paul Joseph Dyson, Gabor Laurenczy, Antoine Philippe Van Muyden, Lu Chen, Xinjiang Cui

A key challenge in the production of lignin-derived chemicals is to reduce the energy intensive processes used in their production. Here, we show that well-defined Rh nanoparticles dispersed in sub-micrometer size carbon hollow spheres, are able to hydroge ...

2020

A One-Step Biofunctionalization Strategy of Electrospun Scaffolds Enables Spatially Selective Presentation of Biological Cues

Silvestro Micera

To recapitulate the heterogeneous complexity of tissues in the human body with synthetic mimics of the extracellular matrix (ECM), it is important to develop methods that can easily allow the selective functionalization of defined spatial domains. Here, a ...

Wiley2020

C/EBP alpha mediates the growth inhibitory effect of progestins on breast cancer cells

Cathrin Brisken, Valentina Scabia

Steroid hormones are key gene regulators in breast cancer cells. While estrogens stimulate cell proliferation, progestins activate a single cell cycle followed by proliferation arrest. Here, we use biochemical and genome-wide approaches to show that proges ...

WILEY2019

New composites for extraction of metal or contaminating chemical species

Wendy Lee Queen, Daniel Teav Sun

he present invention relates to a composite for extracting one or more metal or contaminating chemical species from an aerial or aqueous medium by selective binding, said composite comprising at least one porous template functionalized by at least one poly ...

2019

Hormone receptor signaling in estrogen receptor positive breast cancer

Valentina Scabia

Estrogen receptor (ER) and progesterone receptor (PR) signaling tightly interact in controlling postnatal breast development and impinge on breast carcinogenesis. PR is a direct transcriptional target of ER signaling and ER and PR bind closely to DNA and i ...

EPFL2019

Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity

Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Jeremy Touati, Maola Khan Mohammad Golam, Michal Sabisz, Alice Baumann, Kaycie Marie Butler

Matrix metalloproteinases (MMPs) are zinc‐dependent endopeptidases at the intersection of health and disease due to their involvement in processes such as tissue repair and immunity as well as cancer and inflammation. Because of the high structural conserv ...

2019

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