Kinase Inhibitors for Targeted Cancer Therapy

Precision medicine's quick development has transformed the way cancer is treated, and because small-molecule kinase inhibitors can specifically block the abnormal signaling pathways that cause tumor growth and progression, they are now a key component of targeted therapy. This review explores the most recent advancements in kinase inhibitor design and optimization, with a focus on novel drug scaffolds, improved structure-activity relationships (SARs), and molecular modification techniques meant to improve target selectivity, potency, and pharmacokinetic profiles. Emerging strategies to combat resistance mechanisms are heavily emphasized, such as the use of dual-target inhibitors that block parallel signaling cascades, allosteric modulators that bind to non-ATP sites, and combination therapies that work in concert to increase efficacy while reducing resistance. A thorough summary of the kinase inhibitors that are now FDA-approved for use in treating different forms of cancer is also included in the review, along with information on their safety profiles, clinical effectiveness, and changing indications of usage. Additionally, it examines encouraging results from preclinical research and ongoing clinical studies assessing nextgeneration kinase inhibitors, which have the potential to further customize cancer treatment. In order to improve patient outcomes, address therapeutic resistance, and broaden the therapeutic scope of kinase-targeted interventions in oncology, the review concludes by highlighting future research directions, such as drug repurposing, computational drug discovery, and advanced precision oncology approaches.

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Publication Details

Journal
Current Topics in Medicinal Chemistry
Published
2025-07-30
DOI
https://doi.org/10.2174/0115680266382257250721051440
Primary Topic
Cancer Mechanisms and Therapy
Type
article
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article

Kinase Inhibitors for Targeted Cancer Therapy

Suman Mazumdar, Devalina Ray, M. Amin Mir, Bimal Krishna Banik
Current Topics in Medicinal Chemistry
Cancer Mechanisms and Therapy
article

Kinase Inhibitors for Targeted Cancer Therapy

Suman Mazumdar, Devalina Ray, M. Amin Mir, Bimal Krishna Banik
article en

Abstract

Precision medicine's quick development has transformed the way cancer is treated, and because small-molecule kinase inhibitors can specifically block the abnormal signaling pathways that cause tumor growth and progression, they are now a key component of targeted therapy. This review explores the most recent advancements in kinase inhibitor design and optimization, with a focus on novel drug scaffolds, improved structure-activity relationships (SARs), and molecular modification techniques meant to improve target selectivity, potency, and pharmacokinetic profiles. Emerging strategies to combat resistance mechanisms are heavily emphasized, such as the use of dual-target inhibitors that block parallel signaling cascades, allosteric modulators that bind to non-ATP sites, and combination therapies that work in concert to increase efficacy while reducing resistance. A thorough summary of the kinase inhibitors that are now FDA-approved for use in treating different forms of cancer is also included in the review, along with information on their safety profiles, clinical effectiveness, and changing indications of usage. Additionally, it examines encouraging results from preclinical research and ongoing clinical studies assessing nextgeneration kinase inhibitors, which have the potential to further customize cancer treatment. In order to improve patient outcomes, address therapeutic resistance, and broaden the therapeutic scope of kinase-targeted interventions in oncology, the review concludes by highlighting future research directions, such as drug repurposing, computational drug discovery, and advanced precision oncology approaches.

Current Topics in Medicinal ChemistryVol. 25
Prince Mohammad bin Fahd University (SA), Amity University (IN), Department of Science & Technology (IN)
Good health and well-being
Openalex Percentile: Top 72%
Cancer Mechanisms and Therapy
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Kinase Inhibitors for Targeted Cancer Therapy — Suman Mazumdar, Devalina Ray, et al. · Current Topics in Medicinal Chemistry (2025) | TGRS Research Map | TGRS