Mesenchymal tumor cells drive adaptive resistance of Trp53-/- breast tumor cells to inactivated mutant Kras.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular oncology"
DOI: 10.1002/1878-0261.13220
Abstract: As precision medicine increases the response rate of treatment, tumors frequently bypass inhibition and reoccur. In order for treatment to be effective long term, the mechanisms enabling treatment adaptation need to be understood. Here, we… read more here.
Keywords: treatment; tumor cells; krasg12d; trp53 breast ... See more keywords
Discovery and Characterization of RP03707: A Highly Potent and Selective KRASG12D PROTAC.
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DOI: 10.1021/acs.jmedchem.5c00428
Abstract: KRASG12D, the most prevalent oncogenic mutation in KRAS-associated tumors, represents a highly sought-after drug target for cancer treatment. In this study, we explored a KRASG12D protein degradation approach using the PROTAC technology for the treatment… read more here.
Keywords: discovery characterization; potent selective; selective krasg12d; krasg12d ... See more keywords
ZJK-807: A Selective PROTAC Degrader of KRASG12D Overcoming Resistance in Pancreatic Cancer.
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DOI: 10.1021/acs.jmedchem.5c01034
Abstract: Pancreatic cancer driven by the KRASG12D mutation faces therapeutic challenges from KRAS undruggability and acquired resistance to inhibitors like MRTX1133 via secondary mutations (e.g., Q95/Y96). Here, we report ZJK-807, a novel cereblon (CRBN)-based proteolysis-targeting chimera… read more here.
Keywords: resistance; protac; krasg12d; pancreatic cancer ... See more keywords
Development of thymic tumor in [LSL:KrasG12D; Pdx1-CRE] mice, an adverse effect associated with accelerated pancreatic carcinogenesis
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DOI: 10.1038/s41598-021-94566-x
Abstract: Pancreatic Ductal AdenoCarcinoma (PDAC) represents about 90% of pancreatic cancers. It is one of the most aggressive cancer, with a 5-year survival rate below 10% due to late diagnosis and poor therapeutic efficiency. This bad… read more here.
Keywords: krasg12d pdx1; krasg12d; adverse effect; lsl krasg12d ... See more keywords
Inhibition of GTPase KRASG12D: a review of patent literature
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DOI: 10.1080/13543776.2024.2369630
Abstract: ABSTRACT Introduction KRAS is a critical oncogenic protein intricately involved in tumor progression, and the difficulty in targeting KRAS has led it to be classified as an ‘undruggable target.’ Among the various KRAS mutations, KRASG12D… read more here.
Keywords: gtpase krasg12d; review; inhibition; krasg12d ... See more keywords
KRAS mutation-induced EndMT of brain arteriovenous malformation is mediated through the TGF-β/BMP-SMAD4 pathway
Sign Up to like & getrecommendations! Published in 2022 at "Stroke and Vascular Neurology"
DOI: 10.1136/svn-2022-001700
Abstract: Objective Somatic KRAS mutations have been identified in the majority of brain arteriovenous malformations (bAVMs), and subsequent in vivo experiments have confirmed that KRAS mutation in endothelial cells (ECs) causes AVMs in mouse and zebrafish… read more here.
Keywords: krasg12d; krasg12d mutant; brain arteriovenous; tgf bmp ... See more keywords
Abstract A053: Targeting Acquired Resistance to KRASG12D Inhibitors: designing rationale synergistic treatments
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DOI: 10.1158/1535-7163.targ-25-a053
Abstract: KRASG12D (G12D) is one of the most prevalent and therapeutically challenging oncogenic mutations across pancreatic, colorectal, and lung cancers. The recent development of MRTX1133, a selective, non-covalent G12D inhibitor, represents a major therapeutic breakthrough. Although… read more here.
Keywords: resistance; krasg12d; drug; acquired resistance ... See more keywords
Abstract 24: Oncogenic KrasG12D and Cdkn2a/p16 knockout in LGR5 expressing progenitor cells synergize to advance adenoma and adenocarcinoma phenotypes in murine small intestine
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-24
Abstract: Background: KRAS activating mutations are reported in 42-54% and inactivation of CDKN2A/p16 in 14-30% of human small intestinal adenocarcinomas, suggesting a role in small intestine adenocarcinogenesis. The phenotypic effects of oncogenic KRAS and p16 loss… read more here.
Keywords: krasg12d; cdkn2a p16; small intestine; progenitor cells ... See more keywords
Abstract 4481: Vrtx153, novel small molecule inhibitor of krasg12d
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DOI: 10.1158/1538-7445.am2023-4481
Abstract: Pancreatic cancer is an intractable malignancy and is the seventh leading cause of global cancer deaths in industrialized countries and the third most common in the USA. Despite advancement in the knowledge of potential risk… read more here.
Keywords: vrtx153 novel; krasg12d; inhibitor; novel small ... See more keywords
Abstract LB321: Discovery and characterization of QTX3046, a potent, selective, and orally bioavailable non-covalent KRASG12D inhibitor
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DOI: 10.1158/1538-7445.am2023-lb321
Abstract: The RAS family of proto-oncogenes are the most frequently mutated genes in cancer, in which mutations in KRAS account for approximately 25% of all human cancers. RAS oncogenes impair the ability of RAS to convert… read more here.
Keywords: qtx3046 potent; bioavailable non; krasg12d; orally bioavailable ... See more keywords
Abstract 3315: Preclinical studies of TSN1611, a potent, selective, and orally bioavailable KRASG12D inhibitor
Sign Up to like & getrecommendations! Published in 2024 at "Cancer Research"
DOI: 10.1158/1538-7445.am2024-3315
Abstract: Background: KRAS mutations are the most frequently encountered driver oncogene, involved in ~25% of all human cancers [1,2]. KRASG12D is the predominant KRAS mutation isoform, detected in approximately 35% of pancreatic cancer, 13% of colorectal… read more here.
Keywords: tsn1611 potent; cancer; potent selective; krasg12d ... See more keywords