Abstract
Inappropriate PI3K signaling is one of the most frequent occurrences in human cancer and is critical for tumor progression. A variety of genetic mutations and amplifications have been described affecting key components of this pathway, with implications not only for tumorigenesis but also for resistance to targeted agents. Emerging preclinical research has significantly advanced our understanding of the PI3K pathway and its complex downstream signalling, interactions and crosstalk. This knowledge, combined with the limited clinical antitumor activity of mTOR complex 1 inhibitors, has led to the development of rationally designed drugs targeting key elements of this pathway, such as pure PI3K inhibitors (both pan-PI3K and isoform-specific), dual PI3K/ mTOR inhibitors, Akt inhibitors, and mTOR complexes 1 and 2 catalytic site inhibitors. This review will focus primarily on an analysis of newly developed inhibitors of this pathway that have entered clinical trials, and recently registered patents in this field.
Keywords: Cancer, drug development, mTORC1, mTORC2, PI3K, patent, protein kinase B/Akt
Recent Patents on Anti-Cancer Drug Discovery
Title: Recent Developments in Anti-Cancer Agents Targeting PI3K, Akt and mTORC1/2
Volume: 6 Issue: 2
Author(s): Rodrigo Dienstmann, Jordi Rodon, Ben Markman and Josep Tabernero
Affiliation:
Keywords: Cancer, drug development, mTORC1, mTORC2, PI3K, patent, protein kinase B/Akt
Abstract: Inappropriate PI3K signaling is one of the most frequent occurrences in human cancer and is critical for tumor progression. A variety of genetic mutations and amplifications have been described affecting key components of this pathway, with implications not only for tumorigenesis but also for resistance to targeted agents. Emerging preclinical research has significantly advanced our understanding of the PI3K pathway and its complex downstream signalling, interactions and crosstalk. This knowledge, combined with the limited clinical antitumor activity of mTOR complex 1 inhibitors, has led to the development of rationally designed drugs targeting key elements of this pathway, such as pure PI3K inhibitors (both pan-PI3K and isoform-specific), dual PI3K/ mTOR inhibitors, Akt inhibitors, and mTOR complexes 1 and 2 catalytic site inhibitors. This review will focus primarily on an analysis of newly developed inhibitors of this pathway that have entered clinical trials, and recently registered patents in this field.
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Dienstmann Rodrigo, Rodon Jordi, Markman Ben and Tabernero Josep, Recent Developments in Anti-Cancer Agents Targeting PI3K, Akt and mTORC1/2, Recent Patents on Anti-Cancer Drug Discovery 2011; 6 (2) . https://dx.doi.org/10.2174/157489211795328503
DOI https://dx.doi.org/10.2174/157489211795328503 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...read more
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