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Targeted Protein Degradation: Clinical Advances in the Field of Oncology
The field of targeted protein degradation (TPD) is a rapidly developing therapeutic modality with the promise to tame disease-relevant proteins in ways that are difficult or impossible to tackle with other strategies.
Emilio Casanova, Iris Z Uras
exaly +2 more sources
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Selectivity through Targeted Protein Degradation (TPD).
Journal of medicinal chemistry, 2022Targeted protein degradation has become a reliable tool in the medicinal chemist's toolbox, as seen with rapid progression of PROTACs (proteolysis targeting chimeras) to clinic. Degraders have unique advantages to target proteins with no functional consequence or scaffolding function to achieve the desired phenotype.
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How to target membrane proteins for degradation: Bringing GPCRs into the TPD fold
We are now in the middle of a so-called "fourth wave" of drug innovation: multispecific medicines aimed at diseases and targets previously thought to be "undruggable"; by inducing proximity between two or more proteins, for example, a target and an effector that do not naturally interact, such modalities have potential far beyond the scope of ...
Boguslawa Korona, Laura Itzhaki
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Targeted protein degradation for cancer therapy [PDF]
Targeted protein degradation (TPD) aims at reprogramming the target specificity of the ubiquitin–proteasome system, the major cellular protein disposal machinery, to induce selective ubiquitination and degradation of therapeutically relevant proteins ...
Georg E Winter +2 more
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Targeted protein degradation: current molecular targets, localization, and strategies
Targeted protein degradation (TPD) has revolutionized drug discovery by selectively eliminating specific proteins within and outside the cellular context.
Rainer Riedl
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Cancer Research
Abstract Background: Although three generations of EGFR tyrosine kinase inhibitors (TKIs) have achieved remarkable clinical success, resistance driven by secondary EGFR mutations remains a major therapeutic challenge in non-small cell lung cancer (NSCLC).
Li Zeng, Yao Liu, Ya Geng, Yue Zhu
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Abstract Background: Although three generations of EGFR tyrosine kinase inhibitors (TKIs) have achieved remarkable clinical success, resistance driven by secondary EGFR mutations remains a major therapeutic challenge in non-small cell lung cancer (NSCLC).
Li Zeng, Yao Liu, Ya Geng, Yue Zhu
openaire +1 more source
Targeted protein degradation: A promise for undruggable proteins
Cell Chemical Biology, 2021Kusal T G Samarasinghe, Craig M. Crews
exaly

