Search Results - "Chafiq, Omar Moukha"
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Correction: Tanguturi et al. Discovery of Novel Delta Opioid Receptor (DOR) Inverse Agonist and Irreversible (Non-Competitive) Antagonists. Molecules 2021, 26 , 6693
Published in Molecules (Basel, Switzerland) (18-03-2022)“…There was an error in the original publication [...]…”
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Discovery of Novel Delta Opioid Receptor (DOR) Inverse Agonist and Irreversible (Non-Competitive) Antagonists
Published in Molecules (Basel, Switzerland) (05-11-2021)“…The delta opioid receptor (DOR) is a crucial receptor system that regulates pain, mood, anxiety, and similar mental states. DOR agonists, such as SNC80, and…”
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Effects of SRI-32743, a Novel Quinazoline Structure-Based Compound, on HIV-1 Tat and Cocaine Interaction with Norepinephrine Transporter
Published in International journal of molecular sciences (01-07-2024)“…Prolonged exposure to HIV-1 transactivator of transcription (Tat) protein dysregulates monoamine transmission, a physiological change implicated as a key…”
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A limb-girdle muscular dystrophy 2I model of muscular dystrophy identifies corrective drug compounds for dystroglycanopathies
Published in JCI insight (20-09-2018)Get full text
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Structure–activity relationship for adenosine kinase from Mycobacterium tuberculosis
Published in Biochemical pharmacology (01-04-2008)“…Adenosine kinase (Ado kinase) from Mycobacterium tuberculosis is structurally and biochemically unique from other known Ado kinases. This purine salvage enzyme…”
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The G2019S mutation in LRRK2 imparts resiliency to kinase inhibition
Published in Experimental neurology (01-11-2018)“…The G2019S mutation in LRRK2 is one of the most common known genetic causes of neurodegeneration and Parkinson disease (PD). LRRK2 mutations are thought to…”
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Identification of an Anti-diabetic, Orally Available Small Molecule that Regulates TXNIP Expression and Glucagon Action
Published in Cell metabolism (01-09-2020)“…Diabetes is characterized by hyperglycemia, loss of functional islet beta cell mass, deficiency of glucose-lowering insulin, and persistent alpha cell…”
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Discovery of Novel Delta Opioid Receptor Antagonists
Published in Molecules (Basel, Switzerland) (01-11-2021)“…The delta opioid receptor (DOR) is a crucial receptor system that regulates pain, mood, anxiety, and similar mental states. DOR agonists, such as SNC80, and…”
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The D3 receptor antagonist SR 21502 reduces cue-induced reinstatement of methamphetamine-seeking in rats
Published in Neuroscience letters (29-05-2023)“…•Dopamine D3 receptors play an important role in methamphetamine seeking.•SR 21502 blocks cue-induced reinstatement of methamphetamine seeking in rats.•SR…”
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Inhibition of the SET/MLL Histone Methyltransferase Complex as a Novel Epigenetic Targeted Therapy in Mixed Lineage Leukemia
Published in The FASEB journal (01-05-2021)“…Aggressive acute leukemias in children, adolescents, and adults arise due to a chromosomal translocation and subsequent fusion that occurs at chromosome 11q23…”
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A phase 1 study of NTX-301, an oral DNMT1 inhibitor, in patients with MDS and AML (trial in progress)
Published in Journal of clinical oncology (01-06-2022)“…TPS7077 Background: Patients with relapsed and/or refractory (r/r) myelodysplastic syndrome (MDS), chronic myelomonocytic leukemia (CMML), and acute myeloid…”
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SRI 22136, A Novel Delta Opioid Receptor (DOR) Antagonist for the Treatment of Alzheimer’s Disease
Published in The FASEB journal (01-05-2022)“…Alzheimer’s disease (AD) is the most common form of dementia, which affects 47 million people worldwide. There are over five million AD patients over the age…”
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SRI-32743, a novel allosteric modulator, attenuates HIV-1 Tat protein-induced inhibition of the dopamine transporter and alleviates the potentiation of cocaine reward in HIV-1 Tat transgenic mice
Published in Neuropharmacology (01-12-2022)“…Cocaine abuse increases the incidence of HIV-1-associated neurocognitive disorders. We have demonstrated that HIV-1 transactivator of transcription (Tat)…”
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Parallel Solution-Phase Synthesis and General Biological Activity of a Uridine Antibiotic Analog Library
Published in ACS combinatorial science (12-05-2014)“…A small library of ninety four uridine antibiotic analogs was synthesized, under the Pilot Scale Library (PSL) Program of the NIH Roadmap initiative, from…”
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Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library
Published in European journal of medicinal chemistry (01-03-2020)“…Disruptor of Telomeric Silencing 1-Like (DOT1L), the sole histone H3 lysine 79 (H3K79) methyltransferase, is required for leukemogenic transformation in a…”
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Identification of Quinolinones as Antivirals against Venezuelan Equine Encephalitis Virus
Published in Antimicrobial agents and chemotherapy (17-08-2021)“…Venezuelan equine encephalitis virus (VEEV) is a reemerging alphavirus that can cause encephalitis resulting in severe human morbidity and mortality. Using a…”
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Parallel Solution Phase Synthesis and Preliminary Biological Activity of a 5′-Substituted Cytidine Analog Library
Published in ACS combinatorial science (09-09-2019)“…A 109-membered library of 5′-substituted cytidine analogs was synthesized, via funding through the NIH Roadmap Initiative and the Pilot Scale Library (PSL)…”
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Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors
Published in Journal of medicinal chemistry (22-04-2021)“…A benzo[6]annulene, 4-(tert-butyl)-N-(3-methoxy-5,6,7,8-tetrahydronaphthalen-2-yl) benzamide (1a), was identified as an inhibitor against Chikungunya virus…”
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Studies of the biogenic amine transporters 15. Identification of novel allosteric dopamine transporter ligands with nanomolar potency
Published in The Journal of pharmacology and experimental therapeutics (01-06-2015)“…Novel allosteric modulators of the dopamine transporter (DAT) have been identified. We have shown previously that SRI-9804…”
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Identification of quinazoline compounds as novel potent inhibitors of Wnt/β-catenin signaling in colorectal cancer cells
Published in Oncotarget (08-03-2016)“…The Wnt/β-catenin signaling pathway is critical for the initiation and progression of most colon cancers, and has emerged as one of the most promising targets…”
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