Showing 1-27 of 27 results for "PZ0017"
The mechanism of action of tofacitinib-an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis
Hodge JA, et al.
Clinical and Experimental Rheumatology, 34(2), 318-328 (2016)
Cecilie F Kjelgaard-Petersen et al.
Biochemical pharmacology, 165, 91-98 (2018-07-31)
Currently, there are no disease-modifying osteoarthritis drugs (DMOADs) approved for osteoarthritis. It is hypothesized that a subtype of OA may be driven by inflammation and may benefit from treatment with anti-inflammatory small molecule inhibitors adopted from treatments of rheumatoid arthritis....
Chella Krishna Vadivel et al.
Cancers, 13(2) (2021-01-21)
Perturbation in JAK-STAT signaling has been reported in the pathogenesis of cutaneous T cell lymphoma (CTCL). JAK3 is predominantly associated with the intra-cytoplasmic part of IL-2Rγc located in the plasma membrane of hematopoietic cells. Here we demonstrate that JAK3 is...
Michaela Lang et al.
International journal of cancer, 147(8), 2316-2326 (2020-05-01)
Colorectal cancer is a multifactorial disease involving inherited DNA mutations, environmental factors, gut inflammation and intestinal microbiota. Certain germline mutations within the DNA mismatch repair system are associated with Lynch syndrome tumors including right-sided colorectal cancer with mucinous phenotype and...
Nam Sook Kim et al.
Journal of separation science, 43(14), 2750-2765 (2020-04-17)
An analytical method for the simultaneous and reliable determination of 20 antigout and antiosteoporosis pharmaceutical compounds in adulterated health food products was developed using liquid chromatography with electrospray ionization tandem mass spectrometry and liquid chromatography with quadrupole-time-of-flight mass spectrometry. The...
Zhantao Deng et al.
Biomaterials science, 9(4), 1291-1300 (2020-12-19)
Aseptic loosening is the main reason for surgical revision after arthroplasty. Although a series of mechanisms have been explored, a specific therapeutic target is still desired. In the present study, we explored the role of the signal transducer and activator...
Ben X Wang et al.
Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research, 37(4), 147-152 (2017-04-08)
Aicardi-Goutières syndrome (AGS) is an early-onset, genetic disease characterized by recurrent fever, multifocal lesions of the brain, and systemic autoimmunity. We report on 3 AGS patients, 2 siblings with an RNASEH2A gene mutation and 1 patient with a SAMHD1 gene...
Binding of Janus kinase inhibitor tofacitinib with human serum albumin: multi-technique approach
Abdelhameed AS, et al.
Journal of Biomolecular Structure & Dynamics, 34(9), 2037-2044 (2016)
Brian S Gerstenberger et al.
Scientific reports, 10(1), 8974-8974 (2020-06-04)
Translation of modulation of drug target activity to therapeutic effect is a critical aspect for all drug discovery programs. In this work we describe the profiling of a non-receptor tyrosine-protein kinase (TYK2) inhibitor which shows a functionally relevant potency shift...
Lanhai Lü et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 34(7), 9120-9140 (2020-05-21)
Homeostasis between pro- and anti- inflammatory responses induced by bacteria is critical for the maintenance of health. In the oral cavity, pro-inflammatory mechanisms induced by pathogenic bacteria are well-established; however, the anti-inflammatory responses that act to restrain innate responses remain...
Fernanda O Novais et al.
The Journal of investigative dermatology, 141(3), 575-585 (2020-08-02)
In cutaneous leishmaniasis, the immune response is not only protective but also mediates immunopathology. We previously found that cytolytic CD8 T cells promote inflammatory responses that are difficult to treat with conventional therapies that target the parasite. Therefore, we hypothesized...
Sung Hun Bae et al.
Pharmaceutics, 12(8) (2020-08-06)
Tofacitinib is a Jak inhibitor developed as a treatment for rheumatoid arthritis. Tofacitinib is metabolized mainly through hepatic CYP3A1/2, followed by CYP2C11. Rheumatoid arthritis tends to increase renal toxicity due to drugs used for long-term treatment. In this study, pharmacokinetic...
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Phosphoproteome profiling reveals critical role of JAK-STAT signaling in maintaining chemoresistance in breast cancer
Nascimento AS, et al.
Testing, 8(70), 114756-114756 (2017)
Zhen Li et al.
Frontiers in bioengineering and biotechnology, 8, 583-583 (2020-06-27)
Discogenic low back pain (LBP) is a main cause of disability and inflammation is presumed to be a major driver of symptomatic intervertebral disc degeneration (IDD). Anti-inflammatory agents are currently under investigation as they demonstrated to alleviate symptoms in patients...
Ji Sang Lee et al.
Pharmaceutics, 11(7) (2019-07-10)
This study investigated the pharmacokinetics of tofacitinib in rats and the effects of first-pass metabolism on tofacitinib pharmacokinetics. Intravenous administration of 5, 10, 20, and 50 mg/kg tofacitinib showed that the dose-normalized area under the plasma concentration-time curve from time...
Soumya S Rajan et al.
Oncogene, 39(10), 2103-2117 (2019-12-06)
Rational new strategies are needed to treat tumors resistant to kinase inhibitors. Mechanistic studies of resistance provide fertile ground for development of new approaches. Cancer drug addiction is a paradoxical resistance phenomenon, well-described in MEK-ERK-driven solid tumors, in which drug-target...
L C S De Vries et al.
Inflammatory bowel diseases, 25(4), 647-660 (2019-01-23)
Janus kinases (JAKs) mediate cytokine signaling involved in inflammatory bowel disease. The pan-JAK inhibitor tofacitinib has shown efficacy in the treatment of ulcerative colitis. However, concerns regarding adverse events due to their wide spectrum inhibition fueled efforts to develop selective...
Eun Hye Gwak et al.
Biomolecules & therapeutics, 28(4), 361-369 (2020-03-27)
Tofacitinib, a Janus kinase inhibitor, was developed for the treatment of rheumatoid arthritis. Recently, it has been associated with an increased change in arthritis development in patients with diabetes. Herein, we evaluated the pharmacokinetics of tofacitinib after intravenous (10 mg/kg)...
C Meyer et al.
Clinical and experimental immunology, 181(3), 491-510 (2015-04-24)
In this study we examined the effects of non-myeloablative total body irradiation (TBI) in combination with immunosuppressive chemotherapy on immune homeostasis in rhesus macaques. Our results show that the administration of cyclosporin A or tacrolimus without radiotherapy did not result...
Tofacitinib and TPCA-1 exert chondroprotective effects on extracellular matrix turnover in bovine articular cartilage ex vivo
Kjelgaard-Petersen CF, et al.
Biochemical Pharmacology (2018)
Hozaifa Metwally et al.
Science signaling, 13(624) (2020-03-27)
The lipopolysaccharide (LPS)-induced endocytosis of Toll-like receptor 4 (TLR4) is an essential step in the production of interferon-β (IFN-β), which activates the transcription of antiviral response genes by STAT1 phosphorylated at Tyr701 Here, we showed that STAT1 regulated proinflammatory cytokine...
David Kuo et al.
Science translational medicine, 11(491) (2019-05-10)
Macrophages tailor their function according to the signals found in tissue microenvironments, assuming a wide spectrum of phenotypes. A detailed understanding of macrophage phenotypes in human tissues is limited. Using single-cell RNA sequencing, we defined distinct macrophage subsets in the...
Usir S Younis et al.
AAPS PharmSciTech, 20(5), 167-167 (2019-04-18)
Preformulation studies on tofacitinib citrate, a small molecule JAK3 specific inhibitor, have not been previously reported in literature. We therefore conducted several preformulation studies on tofacitinib citrate, and its free base, to better understand factors that affect its solubility, stability...
Nam Sook Kim et al.
Journal of pharmaceutical and biomedical analysis, 179, 113003-113003 (2019-12-10)
The aim of this study was to simultaneously determine the presence of unauthorized drug substances in health foods and herbal products used in the treatment of conditions such as gout and anti-osteoporosis. Therefore, we developed and optimised a rapid and...
Shiuli Agarwal et al.
Nature communications, 11(1), 6348-6348 (2020-12-15)
Long non-coding RNAs are important regulators of biological processes including immune responses. The immunoregulatory functions of lncRNAs have been revealed primarily in murine models with limited understanding of lncRNAs in human immune responses. Here, we identify lncRNA LUCAT1 which is...
Zhaowei Chen et al.
Science advances, 7(4) (2021-02-02)
Chronic inflammatory diseases often lead to muscle wasting and contractile deficit. While exercise can have anti-inflammatory effects, the underlying mechanisms remain unclear. Here, we used an in vitro tissue-engineered model of human skeletal muscle ("myobundle") to study effects of exercise-mimetic...

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