LAUSR

Mutant-selective topologic conversion facilitates selective degradation of a pathogenic prion isoform

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0 Published in 2019 at "Cell Death and Differentiation"

DOI: 10.1038/s41418-019-0354-1

Abstract: Regulating protein import across the endoplasmic reticulum (ER) membrane occasionally results in the synthesis of topologically unnatural variants, and their accumulation often leads to proteotoxicity. However, since this is a regulated process, it is questionable… read more here.

Keywords: degradation; selective topologic; topologic conversion; prion ... See more keywords

Abstract 1943: SHP2 inhibition as the backbone of targeted therapy combinations for the treatment of cancers driven by oncogenic mutations in the RAS pathway

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2 Published in 2020 at "Cancer Research"

DOI: 10.1158/1538-7445.am2020-1943

Abstract: Direct targeting of oncogenic mutations in the RAS pathway, such as mutant EGFR, BRAFV600E, and most recently KRASG12C, has emerged as a beneficial therapeutic strategy for patients with cancers bearing these mutations. Mutant-selective inhibitors offer… read more here.

Keywords: shp2 inhibition; selective inhibitors; oncogenic mutations; mutations ras ... See more keywords

Abstract 1598: RM-046, a first-in-class, mutant-selective, and oral KRASQ61H(ON) inhibitor that drives tumor regression in preclinical models and validates KRASQ61H as a therapeutic target

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2 Published in 2023 at "Cancer Research"

DOI: 10.1158/1538-7445.am2023-1598

Abstract: KRASQ61H mutant cancers represent a significant unmet medical need and include common solid tumor histotypes such as non-small cell lung cancer (NSCLC), pancreatic ductal adenocarcinoma (PDAC), and colorectal cancer (CRC). Currently, there are no targeted… read more here.

Keywords: cancer; mutant; inhibitor; selective oral ... See more keywords

Computational Approaches for the Design of (Mutant-)Selective Tyrosine Kinase Inhibitors: State-of-the-Art and Future Prospects.

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0 Published in 2020 at "Current topics in medicinal chemistry"

DOI: 10.2174/1568026620666200502005853

Abstract: Kinases remain one of the major attractive therapeutic targets for a large number of indications such as cancer, rheumatoid arthritis, cardiac failure and many others. Design and development of kinase inhibitors (ATP-competitive, allosteric or covalent)… read more here.

Keywords: kinase inhibitors; computational approaches; kinase; selective tyrosine ... See more keywords