Comprehensive review of mechanisms of pathogenesis involved in Alzheimer's disease and potential therapeutic strategies

P Sharma, P Srivastava, A Seth, PN Tripathi… - Progress in …, 2019 - Elsevier
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 …

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 …

[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 …

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 …

Elevated brain cannabinoid CB1 receptor availability in post-traumatic stress disorder: a positron emission tomography study

A Neumeister, MD Normandin, RH Pietrzak… - Molecular …, 2013 - nature.com
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 …

Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects

JZ Long, W Li, L Booker, JJ Burston, SG Kinsey… - Nature chemical …, 2009 - nature.com
Arachidonoylglycerol (2-AG) and anandamide are endocannabinoids that activate the
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 …

Regulation of nausea and vomiting by cannabinoids

LA Parker, EM Rock… - British journal of …, 2011 - Wiley Online Library
Considerable evidence demonstrates that manipulation of the endocannabinoid system
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 …

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 …