Results 131 to 140 of about 4,329 (161)
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Discovery of pyrazoles as novel FPR1 antagonists
Bioorganic and Medicinal Chemistry Letters, 2011A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest.
John Unitt +2 more
exaly +3 more sources
Lead optimisation of pyrazoles as novel FPR1 antagonists
Bioorganic and Medicinal Chemistry Letters, 2012Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with more robust DMPK profiles. These were subsequently improved to generate analogues with attractive overall profiles.
Sarah Lever
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Discovery of small molecule human FPR1 receptor antagonists
Bioorganic and Medicinal Chemistry Letters, 2011The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the ...
John Unitt +2 more
exaly +3 more sources
A TLR3 Ligand Reestablishes Chemotherapeutic Responses in the Context of FPR1 Deficiency
Cancer Discovery, 2021Abstract For anthracycline-based chemotherapy to be immunogenic, dying cancer cells must release annexin A1 (ANXA1) that subsequently interacts with the pattern recognition receptor, formyl peptide receptor 1 (FPR1), on the surface of dendritic cells (DC). Approximately 30% of individuals bear
Peter Vandenabeele +2 more
exaly +5 more sources
FPR1 and Activation of Intestinal Fibroblasts
The FASEB Journal, 2016Fibroblasts are mesenchymal cells that produced the connective tissue consisting of collagens, laminins, and proteoglycans. Myofibroblasts are activated fibroblasts that express α‐smooth muscle actin and contract during wound healing.
Titus A. Reaves +3 more
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FPR1 is essential for rapamycin-induced lifespan extension in Saccharomyces cerevisiae
Biochemical and Biophysical Research Communications, 2023FK506-sensitive proline rotamase 1 protein (Fpr1p), which is a homologue of the mammalian prolyl isomerase FK506-binding protein of 12 kDa (FKBP12), is known to play important roles in protein folding and prevention of protein aggregation. Although rapamycin is known to bind to Fpr1p to inhibit Tor1p mediated-mechanistic Target Of Rapamycin (mTOR ...
Gulperi Yalcin +3 more
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Saccharomyces cerevisiae Fpr1 functions as a chaperone to inhibit protein aggregation
International Journal of Biological Macromolecules, 2021Peptidyl prolyl isomerases (PPIases) accelerate the rate limiting step of protein folding by catalyzing cis/trans isomerization of peptidyl prolyl bonds. The larger PPIases have been shown to be multi-domain proteins, with functions other than isomerization of the proline-containing peptide bond. Recently, a few smaller PPIases have also been described
Eshita, Das +2 more
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FPR1 Blockade And Smoking-Induced Lung Emphysema In Mice
D80. EMPHYSEMA AND COPD: PATHOPHYSIOLOGY, 2012INTRODUCTION: Current dogma supports the concept that airway inflammation is central to the development and progression of chronic obstructive pulmonary disease (COPD) leading to destruction of lung parenchyma as well as alveolar and bronchial tissue remodeling.
LUCATTELLI, MONICA +5 more
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Functional polymorphisms of the FPR1 gene and aggressive periodontitis in Japanese
Biochemical and Biophysical Research Communications, 2007Aggressive periodontitis (AgP), a severe and early onset type of periodontitis, is thought to be subject to significant genetic background effects. Formyl peptide receptor 1 (FPR1) is a gene strongly implicated in AgP. To determine whether variations in this gene are associated with AgP, we performed an association study with 49 AgP patients and 373 ...
Tomohiko, Gunji +10 more
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The Role of FPR1 and GPR32 in Human Inflammation
2015Inflammation is the natural reaction of the body toward tissue injury or pathogen invasion with the ultimate goal to restore homeostasis. When tissue resident APCs sense a perturbation, they release an array of chemokines and signalling molecules, which in turn attract further leukocytes into the affected tissue.
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