Kinase drug discovery 20 years after imatinib: progress and future directions

Philip Cohen; Darren Cross; Pasi A. Jänne

doi:10.1038/s41573-021-00195-4

Kinase drug discovery 20 years after imatinib: progress and future directions

Philip Cohen (Lead / Corresponding author), Darren Cross (Lead / Corresponding author), Pasi A. Jänne (Lead / Corresponding author)

MRC PPU

Research output: Contribution to journal › Review article › peer-review

638 Citations (Scopus)

Abstract

Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery.

Original language	English
Pages (from-to)	551-569
Number of pages	19
Journal	Nature Reviews Drug Discovery
Volume	20
Early online date	17 May 2021
DOIs	https://doi.org/10.1038/s41573-021-00195-4
Publication status	Published - Jul 2021

Keywords

Drug discovery
Drug development
Small molecules

ASJC Scopus subject areas

Drug Discovery
Pharmacology

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1038/s41573-021-00195-4

Cite this

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title = "Kinase drug discovery 20 years after imatinib: progress and future directions",

abstract = "Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery.",

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doi = "10.1038/s41573-021-00195-4",

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T1 - Kinase drug discovery 20 years after imatinib

T2 - progress and future directions

AU - Cohen, Philip

AU - Cross, Darren

AU - Jänne, Pasi A.

PY - 2021/7

Y1 - 2021/7

N2 - Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery.

AB - Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery.

KW - Drug discovery

KW - Drug development

KW - Small molecules

UR - https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8127496/

UR - http://www.scopus.com/inward/record.url?scp=85108401133&partnerID=8YFLogxK

U2 - 10.1038/s41573-021-00195-4

DO - 10.1038/s41573-021-00195-4

M3 - Review article

C2 - 34002056

SN - 1474-1776

VL - 20

SP - 551

EP - 569

JO - Nature Reviews Drug Discovery

JF - Nature Reviews Drug Discovery

ER -

Kinase drug discovery 20 years after imatinib: progress and future directions

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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Elucidation of Mechanisms that Restrict Activation of the Innate Immune System to Prevent Inflammatory and Autoimmune Diseases

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Kinase drug discovery 20 years after imatinib: progress and future directions

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint

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Elucidation of Mechanisms that Restrict Activation of the Innate Immune System to Prevent Inflammatory and Autoimmune Diseases

Cite this