Current advances and development strategies of orally bioavailable PROTACs
S Zeng, Y Ye, H Xia, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …
potential to extend drug space not target to traditional molecules. In the last half decade, we …
Designing soluble PROTACs: strategies and preliminary guidelines
D García Jiménez, M Rossi Sebastiano… - Journal of Medicinal …, 2022 - ACS Publications
Solubility optimization is a crucial step to obtaining oral PROTACs. Here we measured the
thermodynamic solubilities (log S) of 21 commercial PROTACs. Next, we measured BRlogD …
thermodynamic solubilities (log S) of 21 commercial PROTACs. Next, we measured BRlogD …
[HTML][HTML] Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy
In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
Advancing new chemical modalities into clinical studies
MJ Blanco, KM Gardinier… - ACS Medicinal Chemistry …, 2022 - ACS Publications
Drug discovery and development has experienced an incredible paradigm shift in the past
two decades. What once was considered a predominant R&D landscape of small molecules …
two decades. What once was considered a predominant R&D landscape of small molecules …
Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead …
MAM Subbaiah, J Rautio, NA Meanwell - Chemical Society Reviews, 2024 - pubs.rsc.org
The delivery of a drug to a specific organ or tissue at an efficacious concentration is the
pharmacokinetic (PK) hallmark of promoting effective pharmacological action at a target site …
pharmacokinetic (PK) hallmark of promoting effective pharmacological action at a target site …
Targeting the epidermal growth factor receptor with molecular degraders: State-of-the-art and future opportunities
Epidermal growth factor receptor (EGFR) is an oncogenic drug target and plays a critical role
in several cellular functions including cancer cell growth, survival, proliferation …
in several cellular functions including cancer cell growth, survival, proliferation …
Bifunctional degraders of cyclin dependent kinase 9 (CDK9): Probing the relationship between linker length, properties, and selective protein degradation
RJ Tokarski II, CM Sharpe, AC Huntsman… - European Journal of …, 2023 - Elsevier
Abstract Cyclin-dependent kinase 9 (CDK9) is a promising therapeutic target in multiple
cancer types, including acute myeloid leukemia (AML). Protein degraders, also known as …
cancer types, including acute myeloid leukemia (AML). Protein degraders, also known as …
PROTACs: current trends in protein degradation by proteolysis-targeting chimeras
In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …
enormous attention for its ability to overcome the limitations of protein inhibitors and its …
Novel strategies and promising opportunities for targeted protein degradation: An innovative therapeutic approach to overcome cancer resistance
H Zhu, J Wang, Q Zhang, X Pan, J Zhang - Pharmacology & Therapeutics, 2023 - Elsevier
Abstract Targeted Protein Degradation is an emerging and rapidly developing technique for
designing and treating new drugs. With the emergence of a promising class of …
designing and treating new drugs. With the emergence of a promising class of …