Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases?

TY - JOUR

T1 - Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases?

AU - Cohen, Philip

AU - Tcherpakov, Marianna

PY - 2010/11/24

Y1 - 2010/11/24

N2 - Protein phosphorylation and protein ubiquitination regulate most aspects of cell life, and defects in these control mechanisms cause cancer and many other diseases. In the past decade, protein kinases have become one of the most important classes of drug targets for the pharmaceutical industry. In contrast, drug discovery programs that target components of the ubiquitin system have lagged behind. In this Perspective, we discuss the reasons for the delay in this pipeline, the drugs targeting the ubiquitin system that have been developed, and new approaches that may popularize this area of drug discovery in the future.

AB - Protein phosphorylation and protein ubiquitination regulate most aspects of cell life, and defects in these control mechanisms cause cancer and many other diseases. In the past decade, protein kinases have become one of the most important classes of drug targets for the pharmaceutical industry. In contrast, drug discovery programs that target components of the ubiquitin system have lagged behind. In this Perspective, we discuss the reasons for the delay in this pipeline, the drugs targeting the ubiquitin system that have been developed, and new approaches that may popularize this area of drug discovery in the future.

KW - SMALL-MOLECULE INHIBITOR

KW - UNANCHORED POLYUBIQUITIN CHAINS

KW - KAPPA-B ACTIVATION

KW - DEUBIQUITINATING ENZYME

KW - DNA-DAMAGE

KW - LIGASE

KW - PROTEASOME

KW - MDM2

KW - P53

KW - IDENTIFICATION

U2 - 10.1016/j.cell.2010.11.016

DO - 10.1016/j.cell.2010.11.016

M3 - Article

SN - 0092-8674

VL - 143

SP - 686

EP - 693

JO - Cell

JF - Cell

IS - 5

ER -