Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

The race to develop oral SERDs and other novel estrogen receptor inhibitors: recent clinical trial results and impact on treatment options

Y Wang, SC Tang - Cancer and Metastasis Reviews, 2022 - Springer
Hormonal therapy plays a vital part in the treatment of estrogen receptor–positive (ER+)
breast cancer. ER can be activated in a ligand-dependent and independent manner …

Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

S Chen, J Cui, H Chen, B Yu, S Long - European Journal of Medicinal …, 2023 - Elsevier
Targeted protein degradation (TPD) is one of the key strategies of current targeted cancer
therapy, and it can eliminate some of the root causes of cancer, and effectively avoid drug …

Current progress and novel strategies that target CDK12 for drug discovery

P Lei, J Zhang, P Liao, C Ren, J Wang… - European Journal of …, 2022 - Elsevier
CDK12 is a cyclin-dependent kinase that plays critical roles in DNA replication, transcription,
mRNA splicing, and DNA damage repair. CDK12 genomic changes, including mutation …

Molecular glue degraders: exciting opportunities for novel drug discovery

T Lemaitre, M Cornu, F Schwalen, M Since… - Expert Opinion on …, 2024 - Taylor & Francis
ABSTRACT Introduction Molecular Glue Degraders (MGDs) is a concept that refers to a
class of compounds that facilitate the interaction between two proteins or molecules within a …

Protein–Protein Interaction Prediction for Targeted Protein Degradation

O Orasch, N Weber, M Müller, A Amanzadi… - International Journal of …, 2022 - mdpi.com
Protein–protein interactions (PPIs) play a fundamental role in various biological functions;
thus, detecting PPI sites is essential for understanding diseases and developing new drugs …

The emerging role of targeted protein degradation to treat and study cancer

MH Brodermann, EK Henderson… - The Journal of …, 2024 - Wiley Online Library
The evolution of cancer treatment has provided increasingly targeted strategies both in the
upfront and relapsed disease settings. Small‐molecule inhibitors and immunotherapy have …

New approaches for challenging therapeutic targets

KR Sharma, A Malik, RA Roof, JP Boyce… - Drug Discovery Today, 2024 - Elsevier
Despite successes with new drug approvals over the past two decades through
conventional drug development approaches, many human diseases remain intractable to …

Estrogen receptor alpha mutations, truncations, heterodimers, and therapies

GR Hancock, J Gertz, R Jeselsohn… - Endocrinology, 2024 - academic.oup.com
Annual breast cancer (BCa) deaths have declined since its apex in 1989 concomitant with
widespread adoption of hormone therapies that target estrogen receptor alpha (ERα), the …

COVID-19 Therapies: Protease Inhibitions and Novel Degrader Strategies

M Reboud-Ravaux, C El Amri - Frontiers in Drug Discovery, 2022 - frontiersin.org
The global spread of severe acute respiratory syndrome corona virus-2 (SARS-CoV-2)
variants is alarming. In addition to vaccines, effective antiviral agents are urgently needed to …