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Comprehensive review of mechanisms of pathogenesis involved in Alzheimer's disease and potential therapeutic strategies
AD is a progressive neurodegenerative disorder and a leading cause of dementia in an
aging population worldwide. The enormous challenge which AD possesses to global …
aging population worldwide. The enormous challenge which AD possesses to global …
A perspective on the kinetics of covalent and irreversible inhibition
JM Strelow - SLAS Discovery: Advancing Life Sciences R&D, 2017 - journals.sagepub.com
The clinical and commercial success of covalent drugs has prompted a renewed and more
deliberate pursuit of covalent and irreversible mechanisms within drug discovery. A covalent …
deliberate pursuit of covalent and irreversible mechanisms within drug discovery. A covalent …
[HTML][HTML] The role of PPAR alpha in the modulation of innate immunity
M Grabacka, M Pierzchalska, PM Płonka… - International journal of …, 2021 - mdpi.com
Peroxisome proliferator-activated receptor α is a potent regulator of systemic and cellular
metabolism and energy homeostasis, but it also suppresses various inflammatory reactions …
metabolism and energy homeostasis, but it also suppresses various inflammatory reactions …
Identification and Functional Characterization of Brainstem Cannabinoid CB2 Receptors
MD Van Sickle, M Duncan, PJ Kingsley, A Mouihate… - Science, 2005 - science.org
The presence and function of CB2 receptors in central nervous system (CNS) neurons are
controversial. We report the expression of CB2 receptor messenger RNA and protein …
controversial. We report the expression of CB2 receptor messenger RNA and protein …
Elevated brain cannabinoid CB1 receptor availability in post-traumatic stress disorder: a positron emission tomography study
Endocannabinoids and their attending cannabinoid type 1 (CB 1) receptor have been
implicated in animal models of post-traumatic stress disorder (PTSD). However, their specific …
implicated in animal models of post-traumatic stress disorder (PTSD). However, their specific …
Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects
Arachidonoylglycerol (2-AG) and anandamide are endocannabinoids that activate the
cannabinoid receptors CB1 and CB2. Endocannabinoid signaling is terminated by …
cannabinoid receptors CB1 and CB2. Endocannabinoid signaling is terminated by …
Targeting the endocannabinoid system: to enhance or reduce?
V Di Marzo - Nature reviews Drug discovery, 2008 - nature.com
Endocannabinoids are lipid chemical mediators that act locally by activating cannabinoid
receptors of type 1 (CB 1) and type 2 (CB 2) receptors. The two most-studied …
receptors of type 1 (CB 1) and type 2 (CB 2) receptors. The two most-studied …
Regulation of nausea and vomiting by cannabinoids
Considerable evidence demonstrates that manipulation of the endocannabinoid system
regulates nausea and vomiting in humans and other animals. The anti‐emetic effect of …
regulates nausea and vomiting in humans and other animals. The anti‐emetic effect of …
The serine hydrolase ABHD6 controls the accumulation and efficacy of 2-AG at cannabinoid receptors
WR Marrs, JL Blankman, EA Horne, A Thomazeau… - Nature …, 2010 - nature.com
Abstract The endocannabinoid 2-arachidonoylglycerol (2-AG) regulates neurotransmission
and neuroinflammation by activating CB1 cannabinoid receptors on neurons and CB2 …
and neuroinflammation by activating CB1 cannabinoid receptors on neurons and CB2 …
Strategies for discovering and derisking covalent, irreversible enzyme inhibitors
DS Johnson, E Weerapana… - Future medicinal …, 2010 - Taylor & Francis
This article presents several covalent inhibitors, including examples of successful drugs, as
well as highly selective, irreversible inhibitors of emerging therapeutic targets, such as fatty …
well as highly selective, irreversible inhibitors of emerging therapeutic targets, such as fatty …