[HTML][HTML] Phosphoinositide 3-kinase (PI3K) pathway inhibitors in solid tumors: From laboratory to patients
F Janku - Cancer treatment reviews, 2017 - Elsevier
Abstract The phosphoinositide 3-kinase (PI3K) pathway is an intracellular signaling pathway
that has regulatory roles in cell survival, proliferation, and differentiation, and a critical role in …
that has regulatory roles in cell survival, proliferation, and differentiation, and a critical role in …
Protein kinase inhibitors: insights into drug design from structure
MEM Noble, JA Endicott, LN Johnson - Science, 2004 - science.org
Protein kinases are targets for treatment of a number of diseases. This review focuses on
kinase inhibitors that are in the clinic or in clinical trials and for which structural information is …
kinase inhibitors that are in the clinic or in clinical trials and for which structural information is …
Allosteric small-molecule kinase inhibitors
P Wu, MH Clausen, TE Nielsen - Pharmacology & therapeutics, 2015 - Elsevier
Small-molecule kinase inhibitors are invaluable targeted therapeutics for the treatment of
various human diseases, especially cancers. While the majority of approved and developed …
various human diseases, especially cancers. While the majority of approved and developed …
New inhibitors of the PI3K-Akt-mTOR pathway: insights into mTOR signaling from a new generation of Tor Kinase Domain Inhibitors (TORKinibs)
ME Feldman, KM Shokat - Phosphoinositide 3-kinase in Health and …, 2011 - Springer
Abstract mTOR (mammalian Target of Rapamycin) is the hub of the phosphoinositide 3-
Kinase (PI3-K)→ Akt→ mTOR pathway, which is one of the most commonly mutated …
Kinase (PI3-K)→ Akt→ mTOR pathway, which is one of the most commonly mutated …
Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs)
R Roskoski Jr - Pharmacological Research, 2021 - Elsevier
Because dysregulation of protein kinases owing to mutations or overexpression plays
causal roles in human diseases, this family of enzymes has become one of the most …
causal roles in human diseases, this family of enzymes has become one of the most …
Rational therapeutic intervention in cancer: kinases as drug targets
CL Sawyers - Current opinion in genetics & development, 2002 - Elsevier
Landmark clinical studies of new drugs developed to target specific forms of cancer were
reported in 2001. Herceptin, a monoclonal antibody against the Her2/neu receptor tyrosine …
reported in 2001. Herceptin, a monoclonal antibody against the Her2/neu receptor tyrosine …
Biochemical mechanisms of resistance to small-molecule protein kinase inhibitors
R Krishnamurty, DJ Maly - ACS chemical biology, 2010 - ACS Publications
Protein kinases have emerged as one of the most frequently targeted families of proteins in
drug discovery. While the development of small-molecule inhibitors that have the potency …
drug discovery. While the development of small-molecule inhibitors that have the potency …
Through the “gatekeeper door”: exploiting the active kinase conformation
F Zuccotto, E Ardini, E Casale… - Journal of medicinal …, 2010 - ACS Publications
The human genome comprises more than 500 protein kinases including serine/threonine,
tyrosine and dual specificity kinases. 1, 2 Because of the important physiological and …
tyrosine and dual specificity kinases. 1, 2 Because of the important physiological and …
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening
SL McGovern, E Caselli, N Grigorieff… - Journal of medicinal …, 2002 - ACS Publications
High-throughput and virtual screening are widely used to discover novel leads for drug
design. On examination, many screening hits appear non-drug-like: they act …
design. On examination, many screening hits appear non-drug-like: they act …
New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors
V Lamba, I Ghosh - Current pharmaceutical design, 2012 - ingentaconnect.com
Over the past decade, therapeutics that target subsets of the 518 human protein kinases
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …