Trends in kinase drug discovery: targets, indications and inhibitor design
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
PDK1: At the crossroad of cancer signaling pathways
Rational target therapy of cancer would benefit from the identification of new targets that can
be easily inhibited by small molecules. An increasing amount of evidence hints at 3 …
be easily inhibited by small molecules. An increasing amount of evidence hints at 3 …
Allosteric modulator discovery: from serendipity to structure-based design
Allosteric modulators bound to structurally diverse allosteric sites can achieve better
pharmacological advantages than orthosteric ligands. The discovery of allosteric …
pharmacological advantages than orthosteric ligands. The discovery of allosteric …
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 …
Akt kinase activation mechanisms revealed using protein semisynthesis
Akt is a critical protein kinase that drives cancer proliferation, modulates metabolism, and is
activated by C-terminal phosphorylation. The current structural model for Akt activation by C …
activated by C-terminal phosphorylation. The current structural model for Akt activation by C …
Activation of the essential kinase PDK1 by phosphoinositide-driven trans-autophosphorylation
phosphoinositide-dependent kinase 1 (PDK1) is an essential serine/threonine protein
kinase, which plays a crucial role in cell growth and proliferation. It is often referred to as a …
kinase, which plays a crucial role in cell growth and proliferation. It is often referred to as a …
AGC kinases, mechanisms of regulation and innovative drug development
The group of AGC kinases consists of 63 evolutionarily related serine/threonine protein
kinases comprising PDK1, PKB/Akt, SGK, PKC, PRK/PKN, MSK, RSK, S6K, PKA, PKG …
kinases comprising PDK1, PKB/Akt, SGK, PKC, PRK/PKN, MSK, RSK, S6K, PKA, PKG …
Non-kinase targets of protein kinase inhibitors
L Munoz - Nature Reviews Drug Discovery, 2017 - nature.com
Kinome-wide profiling platforms have comprehensively identified the relevant kinases that
are targeted by numerous protein kinase inhibitors. However, recent projects have begun to …
are targeted by numerous protein kinase inhibitors. However, recent projects have begun to …
A therapeutic approach to pantothenate kinase associated neurodegeneration
LK Sharma, C Subramanian, MK Yun, MW Frank… - Nature …, 2018 - nature.com
Pantothenate kinase (PANK) is a metabolic enzyme that regulates cellular coenzyme A
(CoA) levels. There are three human PANK genes, and inactivating mutations in PANK2 …
(CoA) levels. There are three human PANK genes, and inactivating mutations in PANK2 …
Peptide-to-small molecule: a pharmacophore-guided small molecule lead generation strategy from high-affinity macrocyclic peptides
S Yoshida, S Uehara, N Kondo… - Journal of Medicinal …, 2022 - ACS Publications
Recent technological innovations have led to the development of methods for the rapid
identification of high-affinity macrocyclic peptides for a wide range of targets; however, it is …
identification of high-affinity macrocyclic peptides for a wide range of targets; however, it is …