Targeted protein degradation comes of age DOI

Mary E. Matyskiela

Nature Chemical Biology, Journal Year: 2024, Volume and Issue: 21(1), P. 22 - 23

Published: Dec. 24, 2024

Language: Английский

Development of an FKBP12-recruiting chemical-induced proximity DNA-encoded library and its application to discover an autophagy potentiator DOI
Zher Yin Tan,

Joel K.A. Adade,

Xiebin Gu

et al.

Cell chemical biology, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

Language: Английский

Citations

1

The next frontier in drug discovery: Unveiling the pharmacological potential of proximity inducers DOI

Natalie Holmberg‐Douglas,

Katherine E. Near,

Felix González-López de Turiso

et al.

Elsevier eBooks, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

Language: Английский

Citations

0

Targeted protein degradation for cancer therapy DOI
Matthias Hinterndorfer, Valentina A. Spiteri, Alessio Ciulli

et al.

Nature reviews. Cancer, Journal Year: 2025, Volume and Issue: unknown

Published: April 25, 2025

Language: Английский

Citations

0

Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs DOI Creative Commons
Georg E. Winter

ACS Chemical Biology, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 12, 2024

Targeted protein degradation (TPD) is an emerging pharmacologic strategy. It relies on small-molecule "degraders" that induce proximity of a component E3 ubiquitin ligase complex and target to ubiquitination subsequent proteasomal degradation. Essentially, degraders thus expand the function ligases, allowing them degrade proteins they would not recognize in absence small molecule. Over past decade, insights gained from identifying, designing, characterizing various have significantly enhanced our understanding TPD mechanisms, precipitating rational degrader discovery strategies. In this Account, I aim explore how these can be extrapolated anticipate both opportunities challenges utilizing overarching concept proximity-inducing pharmacology manipulate other cellular circuits for dissection biological mechanisms therapeutic purposes.

Language: Английский

Citations

3

New therapies on the horizon: Targeted protein degradation in neuroscience DOI Creative Commons

James A Gregory,

Christopher M. Hickey, Juan D. Chavez

et al.

Cell chemical biology, Journal Year: 2024, Volume and Issue: 31(9), P. 1688 - 1698

Published: Sept. 1, 2024

Language: Английский

Citations

3

Next steps for targeted protein degradation DOI
Mackenzie W. Krone, Craig M. Crews

Cell chemical biology, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 1, 2024

Language: Английский

Citations

3

To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives DOI

Diana Castagna,

Benoit Gourdet,

Roland Hjerpe

et al.

Progress in medicinal chemistry, Journal Year: 2024, Volume and Issue: unknown, P. 61 - 160

Published: Jan. 1, 2024

Language: Английский

Citations

1

Toward target 2035: EUbOPEN - a public–private partnership to enable & unlock biology in the open DOI Creative Commons
Claudia Tredup, Suzanne Ackloo, Hartmut Beck

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 29, 2024

Target 2035 is a global initiative that seeks to identify pharmacological modulator of most human proteins by the year 2035. As part an ongoing series annual updates this initiative, we summarise here efforts EUbOPEN project whose objectives and results are making strong contribution goals public-private partnership with four pillars activity: (1) chemogenomic library collections, (2) chemical probe discovery technology development for hit-to-lead chemistry, (3) profiling bioactive compounds in patient-derived disease assays, (4) collection, storage dissemination project-wide data reagents. The substantial outputs programme include compound covering one third druggable proteome, as well 100 probes, both profiled patient derived hundreds sets deposited existing public repositories project-specific resource exploring outputs.

Language: Английский

Citations

1

Advancements in Protein Degradation for Cancer Therapy DOI Creative Commons
Robert B. Kargbo

ACS Medicinal Chemistry Letters, Journal Year: 2024, Volume and Issue: 15(7), P. 998 - 1000

Published: June 22, 2024

The continuous pursuit of novel therapeutic approaches to modulate biological processes and combat diseases such as cancer has led significant advancements in protein degradation. This Patent Highlight reviews three recent patents introducing innovative compositions methods enhance enzyme activity target These present groundbreaking the development glutarimide-containing compounds Protein-Protein Interaction Targeted Chimeras (PPI-TACs) aimed at improving interventions' efficacy, selectivity, stability.

Language: Английский

Citations

0

Feel the breeze: Opening the therapeutic window with RIPTACs and induced proximity DOI
Kyle Mangano, Patrick Ryan Potts

Cell chemical biology, Journal Year: 2024, Volume and Issue: 31(8), P. 1391 - 1393

Published: Aug. 1, 2024

Language: Английский

Citations

0