Molecular chameleons in drug discovery
V Poongavanam, LHE Wieske, S Peintner… - Nature Reviews …, 2024 - nature.com
Molecular chameleons possess a flexibility that allows them to dynamically shield or expose
polar functionalities in response to the properties of the environment. Although the concept …
polar functionalities in response to the properties of the environment. Although the concept …
[HTML][HTML] Exploring the chemical space of orally bioavailable PROTACs
A principal challenge in the discovery of proteolysis targeting chimeras (PROTACs) as oral
medications is their bioavailability. To facilitate drug design, it is therefore essential to …
medications is their bioavailability. To facilitate drug design, it is therefore essential to …
Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical Landscape
E Price, M Weinheimer, A Rivkin… - Journal of Medicinal …, 2024 - ACS Publications
Developing orally bioavailable drugs demands an understanding of absorption in early drug
development. Traditional methods and physicochemical properties optimize absorption for …
development. Traditional methods and physicochemical properties optimize absorption for …
IMHB-Mediated Chameleonicity in Drug Design: A Focus on Structurally Related PROTACs
D Garcia Jimenez, M Rossi Sebastiano… - Journal of Medicinal …, 2024 - ACS Publications
Molecular chameleonicity may enable compounds to compensate for the unfavorable ADME
properties typically associated with complex molecules, such as PROTACs. Here we present …
properties typically associated with complex molecules, such as PROTACs. Here we present …
Targeted protein degradation in CNS disorders: a promising route to novel therapeutics?
S Kuemper, AG Cairns, K Birchall, Z Yao… - Frontiers in Molecular …, 2024 - frontiersin.org
Targeted protein degradation (TPD) is a rapidly expanding field, with various PROTACs
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …
Conquering the beyond Rule of Five Space with an Optimized High-Throughput Caco-2 Assay to Close Gaps in Absorption Prediction
P Muschong, K Awwad, E Price, M Mezler… - Pharmaceutics, 2024 - mdpi.com
Current drug development tends towards complex chemical molecules, referred to as
“beyond rule of five”(bRo5) compounds, which often exhibit challenging physicochemical …
“beyond rule of five”(bRo5) compounds, which often exhibit challenging physicochemical …
Meeting report: DMPK optimisation strategies and quantitative translational PKPD frameworks to predict human PK and efficacious dose of Targeted protein degraders
C Rynn, HM Duevel - Xenobiotica, 2024 - Taylor & Francis
Targeted protein degradation (TPD), the process of selectively degrading disease-causing
proteins (Lai and Crews 2017), is an emerging and differentiated therapeutic modality that …
proteins (Lai and Crews 2017), is an emerging and differentiated therapeutic modality that …