Search Results - "Mahajan, Sudipta"
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Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases
Published in Journal of medicinal chemistry (24-09-2015)“…While several therapeutic options exist, the need for more effective, safe, and convenient treatment for a variety of autoimmune diseases persists. Targeting…”
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2
STAT signaling in the pathogenesis and treatment of leukemias
Published in Oncogene (25-05-2000)“…Leukemias continue to cause significant mortality in adults and children, and the use of standard cytotoxic chemotherapy has reached a therapeutic plateau…”
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3
Inhibition of MAP Kinase Kinase Causes Morphological Reversion and Dissociation between Soft Agar Growth and in Vivo Tumorigenesis in Angiosarcoma Cells
Published in The American journal of pathology (01-12-2000)“…Activated ras causes increased activity of several signal transduction systems, including the mitogen-activated protein kinase kinase (MAPKK) pathway and the…”
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4
VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease
Published in The Journal of pharmacology and experimental therapeutics (01-05-2015)“…Cytokines, growth factors, and other chemical messengers rely on a class of intracellular nonreceptor tyrosine kinases known as Janus kinases (JAKs) to rapidly…”
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5
Structural Basis for Isoform Selectivity in a Class of Benzothiazole Inhibitors of Phosphoinositide 3‑Kinase γ
Published in Journal of medicinal chemistry (08-01-2015)“…Phosphoinositide 3-kinase γ (PI3Kγ) is an attractive target to potentially treat a range of disease states. Herein, we describe the evolution of a reported…”
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Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3‑Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS)
Published in Journal of medicinal chemistry (28-06-2018)“…The lipid kinase phosphoinositide 3-kinase γ (PI3Kγ) has attracted attention as a potential target to treat a variety of autoimmune disorders, including…”
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7
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3‑Kinase γ
Published in Journal of medicinal chemistry (23-07-2015)“…A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase…”
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8
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors
Published in ACS medicinal chemistry letters (14-01-2021)“…Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation,…”
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9
The Generation and Characterization of a Cell Line Derived from a Sporadic Renal Angiomyolipoma
Published in The American journal of pathology (01-08-2001)“…Angiomyolipomas are benign tumors of the kidney derived from putative perivascular epithelioid cells, that may undergo differentiation into cells with features…”
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10
CRISPR/Cas9 Genome Editing to Treat Sickle Cell Disease and B-Thalassemia: Re-Creating Genetic Variants to Upregulate Fetal Hemoglobin Appear Well-Tolerated, Effective and Durable
Published in Blood (08-12-2017)“…Persistent expression of fetal hemoglobin (HbF) beyond the neonatal period is a rare, naturally-occurring condition, referred to as the Hereditary Persistence…”
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Abstract LB-B15: A novel PI3K gamma isoform selective small molecule kinase inhibitor demonstrates single agent anti-tumor activity and enhanced combination activity with checkpoint blockade in syngeneic mouse models of cancer
Published in Molecular cancer therapeutics (01-12-2015)“…Abstract Immune checkpoint inhibitors have generated impressive clinical responses, however, a number of patients and cancer types remain resistant to…”
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12
Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling
Published in Nature medicine (01-04-1999)“…Fludarabine is a nucleoside analog used in the treatment of hematologic malignancies that can induce severe and prolonged immunosuppression. Although it can be…”
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B lymphocytes from patients with chronic lymphocytic leukemia contain signal transducer and activator of transcription (STAT) 1 and STAT3 constitutively phosphorylated on serine residues
Published in The Journal of clinical investigation (15-12-1997)“…To explore the pathogenesis of chronic lymphocytic leukemia (CLL), we examined whether phosphorylation of one or more signal transducer and activator of…”
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14
Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole
Published in Journal of medicinal chemistry (24-12-2009)“…The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further…”
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15
2-Aminopyrazolo[1,5- a]pyrimidines as potent and selective inhibitors of JAK2
Published in Bioorganic & medicinal chemistry letters (01-12-2009)“…The discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5- a]pyrimidines of potent and selective inhibitors of JAK2 is…”
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16
IL-6-induced survival of colorectal carcinoma cells is inhibited by butyrate through down-regulation of the IL-6 receptor
Published in Carcinogenesis (New York) (01-11-2004)“…Colorectal carcinoma cells are characterized by over-expression of IL-6 and the IL-6 receptor, an autocrine loop that promotes the development of many tumors…”
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17
TEL/PDGFβR fusion protein activates STAT1 and STAT5: A common mechanism for transformation by tyrosine kinase fusion proteins
Published in Experimental hematology (01-05-2000)“…TEL/PDGFβR is a tyrosine kinase fusion protein associated with the pathogenesis of chronic myelomonocytic leukemia. The following experiments were undertaken…”
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18
Altered interleukin-12 responsiveness in Th1 and Th2 cells is associated with the differential activation of stat5 and STAT1
Published in Blood (15-02-1998)“…T-cell activation in response to interleukin-12 (IL-12) is mediated through signaling events that include the tyrosine phosphorylation of STAT4. IL-12…”
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The Generation and Characterization of a Cell Line Derived from a Sporadic Renal Angiomyolipoma : Use of Telomerase to Obtain Stable Populations of Cells from Benign Neoplasms
Published in The American journal of pathology (01-08-2001)“…Angiomyolipomas are benign tumors of the kidney derived from putative perivascular epithelioid cells, that may undergo differentiation into cells with features…”
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20
CD2 stimulation leads to the delayed and prolonged activation of STAT1 in T cells but not NK cells
Published in Experimental hematology (01-02-2001)“…T lymphocytes can be activated by soluble factors such as cytokines or through direct cell-cell interactions. Although cytokine receptors are known to signal…”
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