Search Results - "Van Abbema, Anne"
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Combinatorial efficacy of anti-CS1 monoclonal antibody elotuzumab (HuLuc63) and bortezomib against multiple myeloma
Published in Molecular cancer therapeutics (01-09-2009)“…Monoclonal antibody (mAb) therapy for multiple myeloma, a malignancy of plasma cells, has not been clinically efficacious in part due to a lack of appropriate…”
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Low-dose self-amplifying mRNA COVID-19 vaccine drives strong protective immunity in non-human primates against SARS-CoV-2 infection
Published in Nature communications (07-06-2022)“…The coronavirus disease 2019 (COVID-19) pandemic continues to spread globally, highlighting the urgent need for safe and effective vaccines that could be…”
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CS1, a Potential New Therapeutic Antibody Target for the Treatment of Multiple Myeloma
Published in Clinical cancer research (01-05-2008)“…Purpose: We generated a humanized antibody, HuLuc63, which specifically targets CS1 (CCND3 subset 1, CRACC, and SLAMF7), a cell surface glycoprotein not…”
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A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors
Published in The Journal of immunology (1950) (01-09-2013)“…TYK2 is a JAK family protein tyrosine kinase activated in response to multiple cytokines, including type I IFNs, IL-6, IL-10, IL-12, and IL-23. Extensive…”
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Lead identification of novel and selective TYK2 inhibitors
Published in European journal of medicinal chemistry (01-09-2013)“…A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as psoriasis and inflammatory bowel diseases (IBD), by selective targeting…”
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6
Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors
Published in Journal of medicinal chemistry (26-11-2012)“…The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2…”
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Lead Optimization of a 4‑Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors
Published in Journal of medicinal chemistry (13-06-2013)“…Herein we report our lead optimization effort to identify potent, selective, and orally bioavailable TYK2 inhibitors, starting with lead molecule 3. We used…”
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Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2013)“…A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was…”
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Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2
Published in Bioorganic & medicinal chemistry letters (15-12-2012)“…Herein we describe our successful efforts in obtaining C-2 substituted imidazo-pyrrolopyridines with improved JAK1 selectivity relative to JAK2 by targeting an…”
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Anti-CS1 humanized monoclonal antibody HuLuc63 inhibits myeloma cell adhesion and induces antibody-dependent cellular cytotoxicity in the bone marrow milieu
Published in Blood (15-08-2008)“…Currently, no approved monoclonal antibody (mAb) therapies exist for human multiple myeloma (MM). Here we characterized cell surface CS1 as a novel MM antigen…”
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The neuropeptide Y Y1 antagonist, 1229U91, a potent agonist for the human pancreatic polypeptide-preferring (NPY Y4) receptor
Published in Peptides (New York, N.Y. : 1980) (1998)“…Recently, a novel high-affinity peptide antagonist, 1229U91, was published as a selective neuropeptide Y Y1 antagonist. The selectivity of 1229U91 was…”
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Anti-CSl humanized monoclonal antibody HuLuc63 inhibits myeloma cell adhesion and induces antibody-dependent cellular cytotoxicity in the bone marrow milieu
Published in Blood (15-08-2008)Get full text
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Abstract 724: A novel heterologous prime boost vaccine system drives tumor specific and potent CD8 T cell responses for cancer immunotherapy
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Tumor-specific neoantigens (TSNAs) are present in a majority of tumor types and are key targets for T cells released by immune checkpoint blockade…”
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Identification of Imidazo-Pyrrolopyridines as Novel and Potent JAK1 Inhibitors
Published in Journal of medicinal chemistry (28-06-2012)“…A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as rheumatoid arthritis (RA), by specific targeting of the JAK1 pathway…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Abstract 5379: Inhibition of ULK1/2-mediated autophagy augments antigen processing and presentation in STK11 mutant NSCLC
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract BACKGROUND: Inactivating mutations and deletions in STK11 are present in 9-20% of NSCLC and result in immunologically cold tumors that respond poorly…”
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Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model
Published in Bioorganic & medicinal chemistry letters (15-09-2017)“…[Display omitted] Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through…”
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Identification of C‑2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2
Published in Journal of medicinal chemistry (13-06-2013)“…Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the…”
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Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2
Published in Journal of medicinal chemistry (12-07-2012)“…Herein we report the discovery of the C-2 methyl substituted imidazopyrrolopyridine series and its optimization to provide potent and orally bioavailable JAK1…”
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