Search Results - "Marappan, Sivapriya"
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A highly selective KIT inhibitor MOD000001 suppresses IgE-mediated mast cell activation
Published in The journal of allergy and clinical immunology. Global (01-08-2024)“…The KIT receptor tyrosine kinase and its ligand, stem cell factor (SCF), control proliferation and survival of mast cells. Thus, targeting KIT signaling may…”
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Isolation and purification of a novel antioxidant protein from the water extract of Sundakai ( Solanum torvum) seeds
Published in Food chemistry (2007)“…Reactive oxygen species (ROS) at physiological concentrations may be required for normal cell function. Excessive production of ROS can be detrimental to…”
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Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies
Published in ACS medicinal chemistry letters (10-12-2020)“…Small molecule potent IRAK4 inhibitors from a novel bicyclic heterocycle class were designed and synthesized based on hits identified from Aurigene’s compound…”
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Abstract 1143: Evaluation of AU-18069, a novel small molecule CBP/p300 bromodomain inhibitor for the treatment of cancers
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract Background: E1A binding protein (p300) and its paralog CREB binding protein (CBP or CREBBP) are ubiquitously expressed acetyl transferases (HAT) that…”
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Abstract 1753: Targeting cancer with selective cbp/p300 bromodomain inhibitors
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Background: The Bromodomain (BRD) and Extra-Terminal domain (BET) family of proteins are key regulators of epigenetic control. Although pan BET…”
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Abstract 1754: First in class orally bioavailable BETBRD degraders
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Background: Inhibition of Bromodomain and extra-terminal (BET) family proteins by small molecules is actively being pursued as a therapeutic strategy…”
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Novel CDK12/13 Inhibitors AU-15506 and AU-16770 Are Potent Anti-Cancer Agents in EGFR Mutant Lung Adenocarcinoma with and without Osimertinib Resistance
Published in Cancers (12-04-2023)“…Osimertinib is a third-generation epidermal growth factor receptor and tyrosine kinase inhibitor (EGFR-TKI) approved for the treatment of lung adenocarcinoma…”
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Abstract 4418: Pharmacological characterization of a preclinical candidate covalently inhibiting CDK12
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Cyclin-dependent kinase 12 (CDK12) is a transcription-associated protein that plays a critical role in DNA damage response, splicing, pre-mRNA…”
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Abstract 4649: ODM-207, a novel BET-bromodomain inhibitor as a therapeutic approach for the treatment of prostate and breast cancer
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract Introduction: BET (bromodomain and extraterminal) family proteins (BRD2, BRD3, BRD4, and BRDT) are epigenetic readers that bind to acetylated-lysine…”
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Abstract 118: Targeting cancer with a novel BET bromodomain inhibitor ODM-207
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Abstract Background: Bromodomain and extra-terminal (BET) family proteins are dual bromodomain-containing epigenetic readers that bind to acetylated-lysine…”
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Abstract 2384: Preclinical evaluation of PD and efficacy of novel potent selective and orally bioavailable CDK12 covalent inhibitors in TNBC model
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Cyclin-dependent kinase 12 (CDK12) is a transcription-associated kinase that participates in various cellular processes such as DNA damage response,…”
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Abstract 3303: Paralogue selective p300 degraders induce synthetic lethality in pre-clinical models of CBP-deficient and p300-dependent malignancies
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract EP300 (or p300) acts as histone acetyltransferase (HAT) and transcriptional adapter or co-activator regulating transcription via chromatin remodeling…”
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Abstract 6065: Identification and characterization of paralogue selective CBP degraders for potential use in cancer therapy
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract CBP and p300 are closely related epigenetic modulators that participate in chromatin remodeling and transcription and play an oncogenic role in a…”
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Abstract 3646: Novel IRAK-4 inhibitors exhibit highly potent anti-proliferative activity in DLBCL cell lines with activating MYD88 L265P mutation
Published in Cancer research (Chicago, Ill.) (01-08-2015)“…Abstract Interleukin-1 Receptor Associated Kinase-4 (IRAK-4) is a serine/threonine protein kinase belonging to tyrosine like kinase (TLK) family. IRAK-4 is one…”
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Debio 0617B Inhibits Growth of STAT3-Driven Solid Tumors through Combined Inhibition of JAK, SRC, and Class III/V Receptor Tyrosine Kinases
Published in Molecular cancer therapeutics (01-10-2016)“…Tumor survival, metastases, chemoresistance, and escape from immune responses have been associated with inappropriate activation of STAT3 and/or STAT5 in…”
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Abstract 4798: Efficacy and safety of highly selective novel IRAK4 inhibitors for treatment of ABC-DLBCL
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract Interleukin-1 receptor associated kinases (IRAKs) are serine/threonine protein kinases belonging to the tyrosine-like kinase (TLK) family. IRAKs…”
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Abstract B165: Potent selective and orally bioavailable inhibition of CDK12 by novel covalent inhibitors
Published in Molecular cancer therapeutics (01-01-2018)“…Abstract Background: Cyclin-dependent kinase 12 (CDK12) coordinately regulates the transcription, splicing, and alternative splicing of several large…”
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Abstract B164: Identification of a novel highly selective and orally bioavailable preclinical candidate for CDK7 covalent inhibition
Published in Molecular cancer therapeutics (01-01-2018)“…Abstract Background: Cyclin-dependent kinase 7 (CDK7) is an important constituent of the cellular transcriptional machinery, where it phosphorylates the…”
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Abstract LB-317: Identification of a novel preclinical candidate for CDK7 inhibition
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Abstract Cyclin-dependent kinase 7 (CDK7) is an important constituent of the cellular transcriptional machinery, where it phosphorylates the C-terminal domain…”
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