Search Results - "JAKUBIAK, Diana"
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Blockade of the Phagocytic Receptor MerTK on Tumor-Associated Macrophages Enhances P2X7R-Dependent STING Activation by Tumor-Derived cGAMP
Published in Immunity (Cambridge, Mass.) (18-02-2020)“…Clearance of apoptotic cells by macrophages prevents excessive inflammation and supports immune tolerance. Here, we examined the effect of blocking apoptotic…”
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Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window
Published in Journal of medicinal chemistry (09-06-2016)“…p21-activated kinase 1 (PAK1) has an important role in transducing signals in several oncogenic pathways. The concept of inhibiting this kinase has garnered…”
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P21-Activated Kinase 1 (PAK1) as a Therapeutic Target in BRAF Wild-Type Melanoma
Published in JNCI : Journal of the National Cancer Institute (01-05-2013)“…Although remarkable clinical response rates in melanoma have been observed using vemurafenib or dabrafenib in patients with tumors carrying oncogenic mutations…”
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Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety
Published in ACS medicinal chemistry letters (31-10-2015)“…Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the…”
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Design of Selective PAK1 Inhibitor G‑5555: Improving Properties by Employing an Unorthodox Low‑pK a Polar Moiety
Published in ACS medicinal chemistry letters (10-12-2015)“…Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the…”
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Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900
Published in Molecular cancer therapeutics (01-10-2013)“…Checkpoint kinase 1 (ChK1) is a serine/threonine kinase that functions as a central mediator of the intra-S and G2-M cell-cycle checkpoints. Following DNA…”
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Abstract 944: Development of predictive and pharmacodynamic biomarker strategies for GDC-0425, a checkpoint kinase 1 inhibitor, in combination with gemcitabine
Published in Cancer research (Chicago, Ill.) (01-08-2015)“…Abstract GDC-0425 is a potent and selective small molecule inhibitor of checkpoint kinase 1 (Chk1) recently evaluated in the DPM4957g phase I study in…”
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Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-p K a Polar Moiety
Published in ACS medicinal chemistry letters (10-12-2015)Get full text
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