Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01186
Abstract: Mutations in leucine-rich repeat kinase 2 (LRRK2), such as G2019S, are associated with an increased risk of developing Parkinson's disease. Surrogates for the LRRK2 kinase domain based on checkpoint kinase 1 (CHK1) mutants were designed,… read more here.
Keywords: chk1; leucine rich; kinase; lrrk2 inhibitors ... See more keywords
Impact of Type II LRRK2 inhibitors on signaling and mitophagy
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DOI: 10.1042/bcj20210375
Abstract: Much effort has been devoted to the development of selective inhibitors of the LRRK2 as a potential treatment for LRRK2 driven Parkinson's disease. In this study, we first compare the properties of Type I (GSK3357679A… read more here.
Keywords: type lrrk2; impact type; type inhibitors; lrrk2 inhibitors ... See more keywords
Leucine-rich repeat kinase 2 inhibitors: a patent review (2014-present)
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DOI: 10.1080/13543776.2020.1729354
Abstract: ABSTRACT Introduction: Disease-modifying treatment for Parkinson’s disease (PD) to halt or revert the disease progression remains an unmet medical need. LRRK2 kinase activity is abnormally elevated in PD patients carrying LRRK2 mutations, with G2019S as… read more here.
Keywords: leucine rich; kinase; disease; review ... See more keywords
Structural Insights and Development of LRRK2 Inhibitors for Parkinson’s Disease in the Last Decade
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DOI: 10.3390/genes13081426
Abstract: Parkinson’s disease (PD) is the second most prevalent neurodegenerative disease, characterized by the specific loss of dopaminergic neurons in the midbrain. The pathophysiology of PD is likely caused by a variety of environmental and hereditary… read more here.
Keywords: disease; parkinson disease; lrrk2; development lrrk2 ... See more keywords