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author = "Goffin, Vincent"

Found 13 documents, displaying page 1 of 2

The Addition of Nine Residues at the C-Terminus of Human Prolactin Drastically Alters Its Biological Properties

Description : We have added nine extra residues to the C-terminal of human prolactin and analysed the effect of this mutation on the ability of the hormone to bind to its lactogenic receptor and to induce Nb2 cell division. Both properties are markedly affected when compared to the natural 23-kDa human prolactin....
Repository : ORBi (University of Liège)
Language(s) : English

Evidence for a Second Receptor Binding Site on Human Prolactin

Description : The existence of a second receptor binding site on human prolactin (hPRL) was investigated by site-directed mutagenesis. First, 12 residues of helices 1 and 3 were mutated to alanine. Since none of the resulting mutants exhibit reduced bioactivity in the Nb2 cell proliferation bioassay, the mutated ...
Repository : ORBi (University of Liège)
Language(s) : English

Cathepsin D processes human prolactin into multiple 16K-like N-terminal fragments: Study of their antiangiogenic properties and physiological relevance

Description : 16K prolactin (PRL) is the name given to the 16-kDa N-terminal fragment obtained by proteolysis of rat PRL by tissue extracts or cell lysates, in which cathepsin D was identified as the candidate protease. Based on its antiangiogenic activity, 16K PRL is potentially a physiological inhibitor of tumo...
Repository : ORBi (University of Liège)
Language(s) : English

Solution structure of human prolactin

Description : We report the solution structure of human prolactin determined by NMR spectroscopy. Our result is a significant improvement over a previous structure in terms of number and distribution of distance restraints, regularity of secondary structure, and potential energy. More significantly, the structure...
Repository : ORBi (University of Liège)
Language(s) : English

S179D-human PRL, a pseudophosphorylated human PRL analog, is an agonist and not an antagonist

Description : For many years, our group has been involved in the development of human PRL antagonists. In two recent publications, S179D-human PRL, a human PRL analog designed to mimic a putative S179-phosphorylated human PRL, was reported to be a highly potent antagonist of human PRL-induced proliferation and si...
Repository : ORBi (University of Liège)
Language(s) : English

Polyubiquitination of Prolactin Receptor Stimulates Its Internalization, Postinternalization Sorting, and Degradation via the Lysosomal Pathway▿ †

Description : The ubiquitination of the receptor that mediates signaling induced by the polypeptide pituitary hormone prolactin (PRL) has been shown to lead to the degradation of this receptor and to the ensuing negative regulation of cellular responses to PRL. However, the mechanisms of PRL receptor (PRLr) prote...
Repository : Europe PubMed Central
Language(s) : English

Identification of a gain-of-function mutation of the prolactin receptor in women with benign breast tumors

Description : There is currently no known genetic disease linked to prolactin (Prl) or its receptor (PrlR) in humans. Given the essential role of this hormonal system in breast physiology, we reasoned that genetic anomalies of Prl/PrlR genes may be related to the occurrence of breast diseases with high proliferat...
Repository : Europe PubMed Central
Language(s) : English

Opposing actions of intact and N-terminal fragments of the human prolactin/growth hormone family members on angiogenesis: An efficient mechanism for the regulation of angiogenesis

Description : Angiogenesis, the process of development of a new microvasculature, is regulated by a balance of positive and negative factors. We show both in vivo and in vitro that the members of the human prolactin/growth hormone family, i.e., human prolactin, human growth hormone, human placental lactogen, ...
Repository : Europe PubMed Central
Language(s) : English

Investigation of Prolactin Receptor Activation and Blockade Using Time-Resolved Fluorescence Resonance Energy Transfer

Description : The prolactin receptor (PRLR) is emerging as a therapeutic target in oncology. Knowledge-based drug design led to the development of a pure PRLR antagonist (Del1-9-G129R-hPRL) that was recently shown to prevent PRL-induced mouse prostate tumorogenesis. In humans, the first gain-of-function mutation ...
Repository : Europe PubMed Central
Language(s) : English

Development of pure prolactin receptor antagonists

Description : Prolactin (PRL) promotes tumor growth in various experimental models and leads to prostate hyperplasia and mammary neoplasia in PRL transgenic mice. Increasing experimental evidence argues for the involvement of autocrine PRL in this process. PRL receptor antagonists have been developed to counterac...
Repository : ORBi (University of Liège)
Language(s) : English

Found 13 documents, displaying page 1 of 2