An overview of pim kinase as a target in multiple myeloma.
Sign Up to like & getrecommendations! Published in 2023 at "Cancer medicine"
DOI: 10.1002/cam4.5797
Abstract: Multiple myeloma (MM) is the second common hematologic malignancy manifesting as a clonal proliferation of plasma cells in the bone marrow. In recent years, high expression and activity of pim kinase have been found to… read more here.
Keywords: multiple myeloma; target; pim kinase; kinase ... See more keywords
Uses of dimedone to synthesis pyrazole, isoxazole and thiophene derivatives with antiproliferative, tyrosine kinase and Pim-1 kinase inhibitions
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-020-02579-4
Abstract: We are aiming in this work to synthesize target molecules not only possess antitumor activities but also kinase inhibitors. The target molecules were obtained from dimedone, which reacted with triethoxymethane to produce a product that… read more here.
Keywords: pim kinase; kinase; thiophene; 14b 16b ... See more keywords
A new method for estimating the relative binding free energy, derived from a free energy variational principle for the Pim-1-kinase–ligand and FKBP–ligand systems
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Computer-Aided Molecular Design"
DOI: 10.1007/s10822-020-00302-4
Abstract: In this study, a new method is proposed for calculating the relative binding free energy between a ligand and a protein, derived from a free energy variational principle (FEVP). To address the shortcomings of the… read more here.
Keywords: pim kinase; energy; binding free; ligand ... See more keywords
PIM 3 kinase, a proto-oncogene product, regulates phosphorylation of the measles virus nucleoprotein tail domain at Ser 479 and Ser 510.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.06.002
Abstract: The tail domain of the measles virus (MeV) N protein is typically phosphorylated at S479 and S510. However, the protein kinase responsible for this phosphorylation has not been identified. To identify the protein kinase responsible,… read more here.
Keywords: tail domain; kinase; measles virus; pim kinase ... See more keywords
Pan-PIM kinase inhibitors enhance Lenalidomide's anti-myeloma activity via cereblon-IKZF1/3 cascade.
Sign Up to like & getrecommendations! Published in 2019 at "Cancer letters"
DOI: 10.1016/j.canlet.2018.10.003
Abstract: Multiple myeloma remains an incurable disease, and continued efforts are required to develop novel agents and novel drug combinations with more effective anti-myeloma activity. Here, we show that the pan-PIM kinase inhibitors SGI1776 and CX6258… read more here.
Keywords: pan pim; ikzf1; myeloma; pim kinase ... See more keywords
GW28-e1113 Pim-1 Kinase Phosphorylates Cardiac Troponin I and Regulates Cardiac Myofilament Function
Sign Up to like & getrecommendations! Published in 2017 at "Journal of the American College of Cardiology"
DOI: 10.1016/j.jacc.2017.07.151
Abstract: Pim-1 is a serine/threonine kinase that is highly expressed in the heart, and exerts potent cardiac protective effects through enhancing survival, proliferation, and regeneration of cardiomyocytes. Its myocardial specific substrates, however, remain unknown. In the… read more here.
Keywords: pim kinase; pim; gw28 e1113; kinase ... See more keywords
Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01733
Abstract: Pim kinases are a family of constitutively active serine/threonine kinases that are partially redundant and regulate multiple pathways important for cell growth and survival. In human disease, high expression of the three Pim isoforms has… read more here.
Keywords: methylcyclopropyl; inhibitor; pim kinase; pim ... See more keywords
Safety profiling of genetically engineered Pim-1 kinase overexpression for oncogenicity risk in human c-kit+ cardiac interstitial cells
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DOI: 10.1038/s41434-019-0084-5
Abstract: Advancement of stem cell-based treatment will involve next-generation approaches to enhance therapeutic efficacy which is often modest, particularly in the context of myocardial regenerative therapy. Our group has previously demonstrated the beneficial effect of genetic… read more here.
Keywords: risk; pim kinase; pim; kinase ... See more keywords
Abstract 524: Characterizing thein vitroandin vivoeffects of the PIM kinase inhibitor HS140 in triple-negative human breast cancer
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-524
Abstract: Triple-negative breast cancer (TNBC) lacks expression of the estrogen receptor (ER), the progesterone receptor (PR) and the ERBB2 (also known as HER2) receptor, making it the worse subtype of all breast cancers. Currently, there are… read more here.
Keywords: cancer; breast cancer; triple negative; pim kinase ... See more keywords
Inhibition of PIM kinase with fractionated radiation and docetaxel in preclinical prostate cancer models.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2020.38.15_suppl.e17534
Abstract: e17534Background: PIM kinases are highly expressed in high risk prostate cancer and are associated with aggressiveness and poor prognosis, presenting a therapeutic target. Methods: We studied PIM i... read more here.
Keywords: prostate; inhibition pim; pim kinase; prostate cancer ... See more keywords
Uses of Anthranilic Acid for the Synthesis of Dihydroquinazolin Derivatives with Antitumor, Antiproliferative and Pim-1 kinase Activities.
Sign Up to like & getrecommendations! Published in 2018 at "Acta chimica Slovenica"
DOI: 10.17344/acsi.2017.4146
Abstract: The reaction of anthranilic acid with ethoxycarbonylisothiocyanate gave the ethyl 4-oxo-2-thioxo-1,2-dihydroquinazoline-3(4H)-carboxylate (4). The reaction of compound 4 with hydrazine hydrate and ∆-halocarbonyl derivatives was found to give either hydrazono or S-alkylated products. Heterocyclization reactions of… read more here.
Keywords: pim kinase; dihydroquinazolin derivatives; synthesis dihydroquinazolin; anthranilic acid ... See more keywords