Search Results - "Payan, Donald G."
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1
R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer
Published in Cancer research (Chicago, Ill.) (15-02-2010)“…Accumulating evidence suggests important roles for the receptor tyrosine kinase Axl in cancer progression, invasion, metastasis, drug resistance, and patient…”
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2
Discovery and Development of Spleen Tyrosine Kinase (SYK) Inhibitors
Published in Journal of medicinal chemistry (26-04-2012)Get full text
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3
R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation
Published in The Journal of pharmacology and experimental therapeutics (01-12-2006)“…Recent compelling evidence has lead to renewed interest in the role of antibodies and immune complexes in the pathogenesis of several autoimmune disorders,…”
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4
Developing structure–activity relationships from an HTS hit for inhibition of the Cks1–Skp2 protein–protein interaction
Published in Bioorganic & medicinal chemistry letters (15-11-2015)“…[Display omitted] Structure–activity relationships have been developed around 5-bromo-8-toluylsulfonamidoquinoline 1 a hit compound in an assay for the…”
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5
AMPK activation through mitochondrial regulation results in increased substrate oxidation and improved metabolic parameters in models of diabetes
Published in PloS one (05-12-2013)“…Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein…”
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6
JAK3 Inhibition Significantly Attenuates Psoriasiform Skin Inflammation in CD18 Mutant PL/J Mice
Published in The Journal of immunology (1950) (01-08-2009)“…JAK3, a member of the Janus kinase family, is predominantly expressed in hemopoietic cells and binds specifically to the common gamma chain of a subfamily of…”
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7
Critical role of the ubiquitin ligase activity of UHRF1, a nuclear RING finger protein, in tumor cell growth
Published in Molecular biology of the cell (01-12-2005)“…Early cellular events associated with tumorigenesis often include loss of cell cycle checkpoints or alteration in growth signaling pathways. Identification of…”
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8
The current status and the future of JAK2 inhibitors for the treatment of myeloproliferative diseases
Published in International journal of hematology (01-03-2010)“…Janus kinases (JAKs) are critical components of cytokine signaling pathways which regulate immunity, inflammation, hematopoiesis, growth, and development. The…”
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9
Multiple roles for the receptor tyrosine kinase axl in tumor formation
Published in Cancer research (Chicago, Ill.) (15-10-2005)“…A focus of contemporary cancer therapeutic development is the targeting of both the transformed cell and the supporting cellular microenvironment. Cell…”
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10
Substrate Modification with Lysine 63-linked Ubiquitin Chains through the UBC13-UEV1A Ubiquitin-conjugating Enzyme
Published in The Journal of biological chemistry (12-10-2007)“…Protein modification with lysine 63-linked ubiquitin chains has been implicated in the non-proteolytic regulation of signaling pathways. To understand the…”
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11
R723, a selective JAK2 inhibitor, effectively treats JAK2V617F-induced murine myeloproliferative neoplasm
Published in Blood (23-06-2011)“…The activating mutations in JAK2 (including JAK2V617F) that have been described in patients with myeloproliferative neoplasms (MPNs) are linked directly to MPN…”
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12
Noninvasive imaging of in vivo MuRF1 expression during muscle atrophy
Published in PloS one (01-04-2014)“…Numerous human diseases can lead to atrophy of skeletal muscle, and loss of this tissue has been correlated with increased mortality and morbidity rates…”
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13
Activation of the PKB/AKT Pathway by ICAM-2
Published in Immunity (Cambridge, Mass.) (2002)“…We identified intracellular adhesion molecule-2 (ICAM-2) in a genetic screen as an activator of the PI3K/AKT pathway leading to inhibition of apoptosis. ICAM-2…”
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14
Optimization of Pharmacokinetic and In Vitro Safety Profile of a Series of Pyridine Diamide Indirect AMPK Activators
Published in Journal of medicinal chemistry (28-12-2023)“…A set of focused analogues have been generated around a lead indirect adenosine monophosphate-activated kinase (AMPK) activator to improve the rat clearance of…”
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15
The Poxvirus p28 Virulence Factor Is an E3 Ubiquitin Ligase
Published in The Journal of biological chemistry (24-12-2004)“…A majority of the orthopoxviruses, including the variola virus that causes the dreaded smallpox disease, encode a highly conserved 28-kDa protein with a…”
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16
Bicyclic pyrimidine compounds as potent IRAK4 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-10-2022)“…[Display omitted] Interleukin-1 receptor-associated kinase 4 (IRAK4) plays a critical role in transduction of IL-1R/TLR signaling which is responsible for…”
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17
Discovery of 5‑Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors
Published in ACS medicinal chemistry letters (14-04-2022)“…IRAK4 kinase plays a key role in TLR/IL-1R signaling pathways that regulate innate immune responses, and if uncontrolled, it is responsible for various…”
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18
Retrovirally Delivered Random Cyclic Peptide Libraries Yield Inhibitors of Interleukin-4 Signaling in Human B Cells
Published in The Journal of biological chemistry (04-10-2002)“…Inteins are polypeptide sequences found in a small set of primarily bacterial proteins that promote the splicing of flanking pre-protein sequences to generate…”
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Structure activity relationships leading to the identification of the indirect activator of AMPK, R419
Published in Bioorganic & medicinal chemistry (01-10-2022)“…[Display omitted] Using an in-cell AMPK activation assay, we have developed structure–activity relationships around a hit pyridine dicarboxamide 5 that…”
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20
R-253 Disrupts Microtubule Networks in Multiple Tumor Cell Lines
Published in Clinical cancer research (15-06-2006)“…Purpose: The design and development of synthetic small molecules to disrupt microtubule dynamics is an attractive therapeutic strategy for anticancer drug…”
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