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   Articles with "sos1" as a keyword



PPDPF Promotes the Development of Mutant KRAS‐Driven Pancreatic Ductal Adenocarcinoma by Regulating the GEF Activity of SOS1

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recommendations! Published in 2022 at "Advanced Science"

DOI: 10.1002/advs.202202448

Abstract: The guanine nucleotide exchange factor (GEF) SOS1 catalyzes the exchange of GDP for GTP on RAS. However, regulation of the GEF activity remains elusive. Here, the authors report that PPDPF functions as an important regulator… read more here.

Keywords: sos1; ductal adenocarcinoma; ppdpf; gef activity ... See more keywords
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Structural characterization of 14-3-3ζ in complex with the human Son of sevenless homolog 1 (SOS1).

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recommendations! Published in 2018 at "Journal of structural biology"

DOI: 10.1016/j.jsb.2018.01.011

Abstract: The deviant Ras activation machinery is found in approximately 30% of all human cancers. SOS1 is an important protagonist of this pathway that plays a key-role in aberrant cell proliferation and differentiation. Interaction of SOS1… read more here.

Keywords: complex human; son sevenless; human son; sos1 ... See more keywords

Development of SOS1 Inhibitor-Based Degraders to Target KRAS-Mutant Colorectal Cancer.

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recommendations! Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c01300

Abstract: Direct blockade of KRAS driver mutations in colorectal cancer (CRC) has been challenging. Targeting SOS1, a guanine nucleotide exchange factor, has arisen as an attractive approach for KRAS-mutant CRC. Here, we describe the development of… read more here.

Keywords: sos1; kras mutant; crc; colorectal cancer ... See more keywords

A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRASG12C Inhibitor.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.3c01598

Abstract: AMG510, as the first approved inhibitor for KRASG12C mutation, has shown promising efficacy in nonsmall-cell lung cancer and colorectal cancer harboring KRASG12C mutation. However, the moderate response rate and the rapid emergence of acquired resistance… read more here.

Keywords: sos1; combination; krasg12c inhibitor; efficacy ... See more keywords

Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.3c02433

Abstract: Multitarget medications represent an appealing therapy against the disease with multifactorial abnormalities─cancer. Therefore, simultaneously targeting son of sevenless 1 (SOS1) and epidermal growth factor receptor (EGFR), two aberrantly expressed proteins crucial for the oncogenesis and… read more here.

Keywords: son sevenless; sos1; cancer; prostate cancer ... See more keywords

Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

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recommendations! Published in 2019 at "Proceedings of the National Academy of Sciences of the United States of America"

DOI: 10.1073/pnas.1812963116

Abstract: Significance Mutants of RAS are major oncogenes and occur in many human cancers, but efforts to develop drugs that directly inhibit the corresponding constitutively active RAS proteins have failed so far. We therefore focused on… read more here.

Keywords: inhibitors block; sos1; interaction; sos1 interaction ... See more keywords
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Small molecule Son of Sevenless 1 (SOS1) inhibitors: a review of the patent literature.

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recommendations! Published in 2021 at "Expert opinion on therapeutic patents"

DOI: 10.1080/13543776.2021.1952984

Abstract: IntroductionUp to 30% of all human cancers are driven by the overactivation of RAS signaling. Son of Sevenless 1 (SOS1) is a central node in RAS signaling pathways and modulation of SOS1-mediated RAS activation represents… read more here.

Keywords: son sevenless; small molecule; sos1; sevenless sos1 ... See more keywords

Enhanced expression of son of sevenless homolog 1 is predictive of poor prognosis in uveal malignant melanoma patients

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recommendations! Published in 2019 at "Ophthalmic Genetics"

DOI: 10.1080/13816810.2019.1573904

Abstract: ABSTRACT Purpose: The work outlined herein investigated the prognosis value and the potential role son of sevenless homolog 1 (SOS1) played in uveal melanoma (UM). Methods: We analyzed the mRNA expression level of SOS1 in… read more here.

Keywords: son sevenless; prognosis; expression; sos1 ... See more keywords

The protein kinase complex CBL10–CIPK8–SOS1 functions in Arabidopsis to regulate salt tolerance

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recommendations! Published in 2019 at "Journal of Experimental Botany"

DOI: 10.1093/jxb/erz549

Abstract: Abstract Salt tolerance in plants is mediated by Na+ extrusion from the cytosol by the plasma membrane Na+/H+ antiporter SOS1. This is activated in Arabidopsis root by the protein kinase complex SOS2–SOS3 and in Arabidopsis… read more here.

Keywords: cipk8; sos1; salt tolerance; protein kinase ... See more keywords

PO-173 Critical requirement of the Sos1 and Sos2 RasGEFs for maintenance of mitochondrial homeostasis

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recommendations! Published in 2018 at "ESMO Open"

DOI: 10.1136/esmoopen-2018-eacr25.695

Abstract: Introduction The homologous, ubiquitously expressed, members (Sos1 and Sos2) of the Sos family of RasGEFs participate in multiple signalling pathways but their specific cellular functions are not clearly defined yet. Material and methods Using a… read more here.

Keywords: sos1 dko; sos1 sos2; sos1; sos1 sos1 ... See more keywords

Abstract 1625: A novel SOS1 inhibitor, HM99462 demonstrates antitumor activity against KRAS-mutant cancers

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recommendations! Published in 2023 at "Cancer Research"

DOI: 10.1158/1538-7445.am2023-1625

Abstract: KRAS is a well-known oncogene with the highest mutation rate among various cancers. KRAS cycles between GDP-loaded ‘off’ and GTP-loaded ‘on’ states induce downstream signal transduction to promote cell proliferation and survival. Interconversion between ‘on’… read more here.

Keywords: sos1; hm99462; activity; novel sos1 ... See more keywords