PROTAC and PROTAB: Revolutionizing Cancer Therapy by Targeted Protein Degradation

Chemotherapeutic strategies that target irregularly produced or mutant proteins using monoclonal antibodies (mAbs) and tiny molecular inhibitors have been extensively employed to target cancer. However, because most intracellular proteins lack antigens or active sites with which mAbs or SMIs can engage, they have not been considered druggable targets. After extensive research, PROTACs (Proteolysis Targeting chimaeras) have become a promising way to work with proteins. Scaffolding proteins and transcription factors may also be targeted. The present targets of PROTACs include kinases like CDKs and RTKs, overexpressed oncogenic proteins like AR and BRDs, cancer-driven mutant proteins like EGFR, and disease-relevant fusion proteins like NPM/EML4-ALK and BCR-ABL. The inability of small-molecule intracellular degraders to enter cells and their low bioavailability can also be circumvented with PROTABs. The use of multispecific binding proteins is an improved way to target the breakdown of membrane- bound and cell-surface proteins.

Authors

Institutions

Publication Details

Journal
Clinical Cancer Drugs
Published
2024-11-19
DOI
https://doi.org/10.2174/012212697x323611241109143952
Primary Topic
Protein Degradation and Inhibitors
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

PROTAC and PROTAB: Revolutionizing Cancer Therapy by Targeted Protein Degradation

Swati Verma, Debashish Paramanick, Sarvesh Paliwal
Clinical Cancer Drugs
Protein Degradation and Inhibitors
article

PROTAC and PROTAB: Revolutionizing Cancer Therapy by Targeted Protein Degradation

Swati Verma, Debashish Paramanick, Sarvesh Paliwal
article en

Abstract

Chemotherapeutic strategies that target irregularly produced or mutant proteins using monoclonal antibodies (mAbs) and tiny molecular inhibitors have been extensively employed to target cancer. However, because most intracellular proteins lack antigens or active sites with which mAbs or SMIs can engage, they have not been considered druggable targets. After extensive research, PROTACs (Proteolysis Targeting chimaeras) have become a promising way to work with proteins. Scaffolding proteins and transcription factors may also be targeted. The present targets of PROTACs include kinases like CDKs and RTKs, overexpressed oncogenic proteins like AR and BRDs, cancer-driven mutant proteins like EGFR, and disease-relevant fusion proteins like NPM/EML4-ALK and BCR-ABL. The inability of small-molecule intracellular degraders to enter cells and their low bioavailability can also be circumvented with PROTABs. The use of multispecific binding proteins is an improved way to target the breakdown of membrane- bound and cell-surface proteins.

Clinical Cancer DrugsVol. 10
Banasthali University (IN), Institute of Management Technology (IN), KR Mangalam University (IN)
Good health and well-being
Openalex Percentile: Top 81%
Protein Degradation and Inhibitors
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.

PROTAC and PROTAB: Revolutionizing Cancer Therapy by Targeted Protein Degradation — Swati Verma, Debashish Paramanick, et al. · Clinical Cancer Drugs (2024) | TGRS Research Map | TGRS