Search Results - "Gore, Suraj T."
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Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders
Published in Bioorganic & medicinal chemistry letters (01-01-2022)“…[Display omitted] Multiple Splice variants of AR have been reported in the past few years. These splice variants are upregulated in most cases of CRPC…”
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Plasmodium chitinases: revisiting a target of transmission‐blockade against malaria
Published in Protein science (01-08-2021)“…Malaria is a life‐threatening disease caused by one of the five species of Plasmodium, among which Plasmodium falciparum cause the deadliest form of the…”
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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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Design, Synthesis and Pharmacological Screening of Novel Antihypertensive Agents Using Hybrid Approach
Published in Bioorganic & medicinal chemistry (2009)“…Eight derivatives of general formula 2-(2-(4-(3-((5-substituted…”
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Design, synthesis and pharmacological screening of novel nitric oxide donors containing 1,5-diarylpyrazolin-3-one as nontoxic NSAIDs
Published in European journal of medicinal chemistry (01-11-2009)“…Various substituted 1,5-diarylpyrazol-3-one derivatives were synthesized and screened for analgesic, anti-inflammatory activities, ulcerogenic potential and…”
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Abstract 1144: Orally bioavailable SMARCA2 degraders with exceptional selectivity and potency
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract Background: SMARCA2 (BRM) and SMARCA4 (BRG1) are two mutually exclusive DNA-dependent ATPases of the SWI/SNF complex, which function in mobilizing…”
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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 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 3729: Discovery of orally bioavailable SMARCA2/4 dual degraders for treatment of acute myeloid leukemia
Published in Cancer research (Chicago, Ill.) (15-06-2022)“…Abstract Background: The BAF (SWI/SNF) chromatin remodeling complex comprises of two mutually exclusive ATPases, SMARCA2 (BRM) and SMARCA4 (BRG1), that affect…”
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Abstract 4114: Evaluation of AU-18069, a novel small molecule CBP/p300 bromodomain inhibitor for the treatment of cancers
Published in Cancer research (Chicago, Ill.) (15-06-2022)“…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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