Search Results - "Arjun Surya"
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The discovery of potent small molecule activators of human STING
Published in European journal of medicinal chemistry (01-01-2021)“…The adaptor protein STING plays a major role in innate immune sensing of cytosolic nucleic acids, by triggering a robust interferon response. Despite the…”
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G10 is a direct activator of human STING
Published in PloS one (10-09-2020)“…The cGAS/STING pathway initiates an innate immune response when DNA is detected in the cytosol. DNA bound cGAS synthesizes cyclic dinucleotides which bind and…”
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782-D Systemic delivery of novel, allosteric STING agonist CRD3874-SI leads to robust anti-cancer activity by generating pro-inflammatory Type I IFN signals while blocking proton channel mediated toxicity
Published in Journal for immunotherapy of cancer (01-11-2023)“…BackgroundSTING activates Type1 interferon and pro-inflammatory responses to drive anti-tumor immunity. Current STING agonists under clinical investigation…”
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Transducin Activation by the Bovine Opsin Apoprotein (∗)
Published in The Journal of biological chemistry (10-03-1995)“…The interaction of the bovine opsin apoprotein with transducin in rod outer segment membranes was investigated using a guanyl nucleotide exchange assay. In…”
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Molecular cloning and pharmacological characterization of bovine calcitonin receptor-like receptor from bovine aortic endothelial cells
Published in Biochemical pharmacology (01-06-2002)“…A complementary DNA encoding calcitonin receptor-like receptor (CRLR) was isolated from a bovine aortic endothelial cell library. The bovine CRLR has 462 amino…”
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The discovery of potent small molecule cyclic urea activators of STING
Published in European journal of medicinal chemistry (05-02-2022)“…STING mediates innate immune responses that are triggered by the presence of cytosolic DNA. Activation of STING to boost antigen recognition is a therapeutic…”
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Modulation of Opsin Apoprotein Activity by Retinal
Published in The Journal of biological chemistry (29-08-1997)“…The bovine opsin apoprotein activates transducin, although at a much reduced level than light-activated rhodopsin (Surya, A., Foster, K., and Knox, B. (1995)…”
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Light-dependent Activation of Rod Transducin by Pineal Opsin
Published in The Journal of biological chemistry (09-10-1998)“…The pineal gland expresses a unique member of the opsin family (P-opsin; Max, M., McKinnon, P. J., Seidenman, K. J., Barrett, R. K., Applebury, M. L.,…”
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Enhancement of Opsin Activity by all-trans-retinal
Published in Experimental eye research (01-05-1998)“…The rod cell photoreceptor apoprotein, opsin, activates the G-protein, transducin, although at a much reduced level than light-activated rhodopsin. The ability…”
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Abstract 5322: Discovery of CRD1601, a potent and selective HPK1 inhibitor with robust in vivo anti-cancer activity
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Background: Haematopoietic Progenitor Kinase (HPK-1, MAP4K1) is a member of the STE20 family of serine/threonine kinases, expressed predominantly in…”
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Abstract LB-061: CRD5500: A versatile small molecule STING agonist amenable to bioconjugation as an ADC
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…BACKGROUND Innate immune signaling mediated through STING (Stimulator of Interferon Genes) generates a Type I interferon (Type 1 IFN) signal that increases T…”
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Abstract 3510: Small molecule ACSS2 inhibitors target acetate metabolizing tumor cells in hypoxic conditions
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…BACKGROUND Tumors such as glioblastoma proliferating under hypoxic, hypoglycemic and hypolipidemic conditions derive almost half of their nutritional…”
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Temozolomide analogs with improved brain/plasma ratios – Exploring the possibility of enhancing the therapeutic index of temozolomide
Published in Bioorganic & medicinal chemistry letters (15-10-2016)“…[Display omitted] Temozolomide is a chemotherapeutic agent that is used in the treatment of glioblastoma and other malignant gliomas. It acts through DNA…”
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Abstract 7481: The allosteric STING agonist CRD3874 is systemically tolerated demonstrates systemic tolerability
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Background: The activation of STING by CDN bind site targeting ligands leads to the generation of Type I interferons as well as pyroptosis and autophagy of the…”
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Abstract 1996: Intravenous administration of the small molecule STING agonist CRD5500 elicits potent anti-tumor immune responses in cold tumors
Published in Cancer research (Chicago, Ill.) (15-06-2022)“…Background: Innate immune signaling mediated through STING (Stimulator of Interferon Genes) generates a Type I interferon (Type 1 IFN) signal that increases T…”
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Abstract 2122: CRD1600 is a potent HPK-I inhibitor with robust immune modulatory properties
Published in Cancer research (Chicago, Ill.) (15-06-2022)“…Background: Haematopoietic Progenitor Kinase (HPK-1, MAP4K1) is a member of the STE20 family of serine/threonine kinases, expressed predominantly in…”
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G10 is a direct activator of human STING
Published in PloS one (01-01-2020)“…The cGAS/STING pathway initiates an innate immune response when DNA is detected in the cytosol. DNA bound cGAS synthesizes cyclic dinucleotides which bind and…”
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Abstract LB-085: RG70099: A novel, highly potent dual IDO1/TDO inhibitor to reverse metabolic suppression of immune cells in the tumor micro-environment
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…IDO1/TDO* mediate substantial immunosuppressive effects through the metabolism of tryptophan (Trp) to kynurenine (Kyn). The consequent decrease in Trp…”
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Abstract LB-085: RG70099: A novel, highly potent dual IDO1TDO inhibitor to reverse metabolic suppression of immune cells in the tumor micro-environment
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…IDO1TDO mediate substantial immunosuppressive effects through the metabolism of tryptophan (Trp) to kynurenine (Kyn). The consequent decrease in Trp suppresses…”
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Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ
Published in ACS medicinal chemistry letters (08-12-2016)“…The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3Kδ are kinases responsible for…”
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