Targeting KRAS in Colorectal Cancer
Sign Up to like & getrecommendations! Published in 2021 at "Current Oncology Reports"
DOI: 10.1007/s11912-021-01022-0
Abstract: Mutations in kirsten rat sarcoma viral oncogene homolog (KRAS) are the most frequently observed genomic alterations in human cancers. No KRAS targeting therapy has been approved despite more than three decades of efforts. Encouraging progress… read more here.
Keywords: krasg12c; colorectal cancer; targeting kras; kras colorectal ... See more keywords
D-1553: A novel KRASG12C inhibitor with potent and selective cellular and in vivo antitumor activity.
Sign Up to like & getrecommendations! Published in 2023 at "Cancer science"
DOI: 10.1111/cas.15829
Abstract: D-1553 is a small molecule inhibitor selectively targeting KRASG12C and currently in phase II clinical trials. Here, we report the preclinical data demonstrating antitumor activity of D-1553. Potency and specificity of D-1553 in inhibiting GDP-bound… read more here.
Keywords: antitumor activity; krasg12c; activity 1553; inhibitor ... See more keywords
AZD4625 is a Potent and Selective Inhibitor of KRASG12C
Sign Up to like & getrecommendations! Published in 2022 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-22-0241
Abstract: Abstract AZD4625 is a potent, selective, and orally bioavailable inhibitor of oncogenic KRASG12C as demonstrated in cellular assays and in vivo in preclinical cell line–derived and patient-derived xenograft models. In vitro and cellular assays have… read more here.
Keywords: inhibitor krasg12c; krasg12c; selective inhibitor; azd4625 potent ... See more keywords
Bcl-xL Is a Key Mediator of Apoptosis Following KRASG12C Inhibition in KRASG12C-mutant Colorectal Cancer
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DOI: 10.1158/1535-7163.mct-22-0301
Abstract: Purpose Novel covalent inhibitors of KRASG12C have shown limited response rates in KRASG12C mutant (MT) colorectal cancer (CRC) patients. Thus, novel KRASG12C inhibitor combination strategies that can achieve deep and durable responses are needed. Experimental… read more here.
Keywords: cancer; apoptosis; mutant colorectal; krasg12c ... See more keywords
Abstract 1142: Discovery of FMC-376 a novel orally bioavailable inhibitor of activated KRASG12C
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-1142
Abstract: KRAS is one of the most frequently mutated genes in cancer and was long considered undruggable until the recent discovery of inhibitors that bind the inactive (GDP-bound) form of KRASG12C. The most clinically advanced of… read more here.
Keywords: discovery fmc; 376 novel; fmc 376; inhibitor ... See more keywords
Abstract 2692: The combination of ulixertinib (ERK1/2 Inhibitor) and KRASG12C inhibition demonstrates significant efficacy in preclinical models
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-2692
Abstract: Ulixertinib (BVD-523) is a first-in-class and best-in-class small molecule inhibitor of ERK1/2 currently being investigated in several oncology clinical trials, both as a single agent and in combination with other therapeutics. Ulixertinib has demonstrated efficacy… read more here.
Keywords: inhibition; combination; inhibitor; efficacy ... See more keywords
Abstract 3448: Discovery of HYP-2A,a 2nd- generation KRASG12C inhibitor exhibits potent in vivo efficacy in drug resistant tumor models
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3448
Abstract: Although activating mutations in KRAS are well recognized as a hallmark of cancer, KRAS was considered an undruggable target for over 30 years after its discovery, due to the intrinsic characteristics of KRAS proteins. The… read more here.
Keywords: hyp; krasg12c inhibitor; efficacy; krasg12c ... See more keywords
Abstract 3638: Integrated single-cell and spatial analysis reveal the mechanism of KRASG12C inhibitor AMG510 in HSC-humanized NOG-EXL model
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-3638
Abstract: Background: Intra-tumor heterogeneity is one of the biggest challenges in cancer treatment today. Current single-cell RNA sequencing technologies itself could enable the exploration of gene expression heterogeneity at the single cell level, but they cannot… read more here.
Keywords: cell; amg510; krasg12c; single cell ... See more keywords
Abstract 412: Drug combination screen identifies pemigatinib, an FGFR inhibitor, as a mechanism to overcome KRASG12C inhibitor resistance in lung cancer
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-412
Abstract: Background: Lung cancer is one of the most common tumors, accounting for approximately 1.8 million deaths worldwide in 2020. KRAS is a frequently mutated oncogene, with mutations reported in roughly 20-25% of non-small cell lung… read more here.
Keywords: lung cancer; combination; inhibitor; krasg12c ... See more keywords
Abstract 430: Pemigatinib, an FGFR inhibitor, overcomes resistance to KRASG12C inhibitors in mesenchymal-like NSCLC tumors
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DOI: 10.1158/1538-7445.am2023-430
Abstract: KRAS is one of the most frequently mutated oncogenes. Clinical studies with recently developed covalent KRASG12C inhibitors have shown promising anticancer activity in patients with KRASG12C tumors (substitution of glycine to cysteine at amino acid… read more here.
Keywords: expression; mesenchymal like; krasg12c inhibitors; krasg12c ... See more keywords
Abstract LB316: A next-generation KRASG12C inhibitor ABSK071 demonstrated broad synergy with other therapeutic agents in KRASG12C mutated cancer models
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DOI: 10.1158/1538-7445.am2023-lb316
Abstract: Background: KRAS is frequently mutated in human cancers, including pancreatic (~90%), colorectal (~35%), and lung cancer (~25%). The KRASG12C mutation (single amino acid substitution of cysteine for glycine at position 12) accounts for ~14% of… read more here.
Keywords: absk071; inhibitor; krasg12c; next generation ... See more keywords