Peter Greb
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View article: Frustration in the Protein-Protein interface Plays a Central Role in the Cooperativity of PROTAC Ternary Complexes
Frustration in the Protein-Protein interface Plays a Central Role in the Cooperativity of PROTAC Ternary Complexes Open
Targeted protein degradation of a protein of interest (POI) by Proteolysis Targeting Chimeras (PROTACs) is an attractive approach for dealing with formerly undruggable protein targets. PROTACs are heterobifunctional molecules that connect …
View article: Confounding Factors in Targeted Degradation of Short-Lived Proteins
Confounding Factors in Targeted Degradation of Short-Lived Proteins Open
Targeted protein degradation has recently emerged as a novel option in drug discovery. Natural protein half-life is expected to affect the efficacy of degrading agents, but to what extent it influences target protein degradation has not be…
View article: Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria
Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria Open
Antimicrobial resistance is a global health threat that requires the development of new treatment concepts. These should not only overcome existing resistance but be designed to slow down the emergence of new resistance mechanisms. Targete…
View article: Confounding factors in targeted degradation of short-lived proteins
Confounding factors in targeted degradation of short-lived proteins Open
Summary Targeted protein degradation has recently emerged as a novel option in drug discovery. Natural protein half-life is expected to affect the efficacy of degrading agents, but to what extent it influences target protein degradation ha…
View article: Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria
Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria Open
Antimicrobial resistance is a global health threat that requires development of new treatment concepts. These should not only overcome existing resistance, but be designed to slow down emergence of new resistance mechanisms. Targeted prote…
View article: Drugit: Crowd-sourcing molecular design of non-peptidic VHL binders
Drugit: Crowd-sourcing molecular design of non-peptidic VHL binders Open
Given the role of human intuition in current drug design efforts, crowd-sourced 'citizen scientist' games have the potential to greatly expand the pool of potential drug designers. Here, we introduce ‘Drugit', the small molecule design mod…
View article: BacPROTAC-induced degradation of ClpC1 as a new strategy against drug-resistant mycobacteria
BacPROTAC-induced degradation of ClpC1 as a new strategy against drug-resistant mycobacteria Open
Antimicrobial resistance (AMR) is a global public health threat that urgently requires development of new treatment concepts. In general, these treatments should not only be able to overcome existing resistance, but designed to slow down o…
View article: A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo Open
Targeted protein degradation offers an alternative modality to classical inhibition and holds the promise of addressing previously undruggable targets to provide novel therapeutic options for patients. Heterobifunctional molecules co-recru…
View article: Reply to Tran et al.: Dimeric KRAS protein–protein interaction stabilizers
Reply to Tran et al.: Dimeric KRAS protein–protein interaction stabilizers Open
We thank Tran et al. (1) for their appreciation of our open innovation platform (https://opnme.com/) and interest in our manuscript (2) in which we demonstrate that the small-molecule KRAS inhibitor BI-2852 reduces pERK (EC50 = 6 µM) and i…
View article: Drugging an undruggable pocket on KRAS
Drugging an undruggable pocket on KRAS Open
The 3 human RAS genes, KRAS, NRAS, and HRAS, encode 4 different RAS proteins which belong to the protein family of small GTPases that function as binary molecular switches involved in cell signaling. Activating mutations in RAS are among t…
View article: Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions
Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions Open
Focal adhesion tyrosine kinase (PTK2) is often overexpressed in human hepatocellular carcinoma (HCC), and several reports have linked PTK2 depletion and/or pharmacological inhibition to reduced tumorigenicity. However, the clinical relevan…
View article: Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6
Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6 Open
The transcription factor BCL6 is a known driver of oncogenesis in lymphoid malignancies, including diffuse large B cell lymphoma (DLBCL). Disruption of its interaction with transcriptional repressors interferes with the oncogenic effects o…