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Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer's drugs targeting acetyl- and butyryl-cholinesterase.
The multifunctional nature of Alzheimer's disease calls for MTDLs (multitarget-directed ligands) to act on different components of the pathology, like the cholinergic dysfunction and amyloidExpand
Structure, activities and biomedical applications of human butyrylcholinesterase.
Human butyrylcholinesterase (BuChE) is a serine enzyme present in most organs and plasma. No clear physiological function has yet been assigned to BuChE, but it is a pharmacologically andExpand
Structural evidence that human acetylcholinesterase inhibited by tabun ages through O-dealkylation.
Tabun is a warfare agent that inhibits human acetylcholinesterase (hAChE) by rapid phosphylation of the catalytic serine. A time-dependent reaction occurs on the tabun adduct, leading to an "aged"Expand
Reactibodies generated by kinetic selection couple chemical reactivity with favorable protein dynamics
Igs offer a versatile template for combinatorial and rational design approaches to the de novo creation of catalytically active proteins. We have used a covalent capture selection strategy toExpand
The marine natural product adociasulfate-2 as a tool to identify the MT-binding region of kinesins.
Kinesins are molecular motors that transport cargo along microtubules (MTs). To move forward the motor must attach to the MT in a defined orientation and detach from it in a process that is driven byExpand
Aging of cholinesterases phosphylated by tabun proceeds through O-dealkylation.
Human butyrylcholinesterase (hBChE) hydrolyzes or scavenges a wide range of toxic esters, including heroin, cocaine, carbamate pesticides, organophosphorus pesticides, and nerve agents.Expand
Structure-activity analysis of aging and reactivation of human butyrylcholinesterase inhibited by analogues of tabun.
hBChE [human BChE (butyrylcholinesterase)] naturally scavenges OPs (organophosphates). This bioscavenger is currently in Clinical Phase I for pretreatment of OP intoxication. Phosphylated ChEsExpand
Structural Study of the Complex Stereoselectivity of Human Butyrylcholinesterase for the Neurotoxic V-agents*
Nerve agents are chiral organophosphate compounds (OPs) that exert their acute toxicity by phosphorylating the catalytic serine of acetylcholinesterase (AChE). The inhibited cholinesterases can beExpand
A novel miR-371a-5p-mediated pathway, leading to BAG3 upregulation in cardiomyocytes in response to epinephrine, is lost in Takotsubo cardiomyopathy
Molecular mechanisms protecting cardiomyocytes from stress-induced death, including tension stress, are essential for cardiac physiology and defects in these protective mechanisms can result inExpand
Huprine Derivatives as Sub‐Nanomolar Human Acetylcholinesterase Inhibitors: From Rational Design to Validation by X‐ray Crystallography
Alzheimer’s disease (AD) is the most common cause of senile dementia. Because of its dramatic human and economic impact, it has become one of the major public health issues of the 21st Century, withExpand