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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
Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance.
Graphical Abstract Highlights d HA15 is a molecule that targets specifically BiP/GRP78/ HSPA5 d HA15 induces ER stress leading to cancer cell death in vitro and in vivo d HA15 overcomes BRAFExpand
Human butyrylcholinesterase produced in insect cells: huprine‐based affinity purification and crystal structure
Butyrylcholinesterase (BChE) is a serine hydrolase that is present in all mammalian tissues. It can accommodate larger substrates or inhibitors than acetylcholinesterase (AChE), the enzymeExpand
ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer stem cells.
DNA inevitably undergoes a high number of damages throughout the cell cycle. To preserve the integrity of the genome, cells have developed a complex enzymatic machinery aimed at sensing and repairingExpand
Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance.
We have discovered and developed a series of molecules (thiazole benzenesulfonamides). HA15, the lead compound of this series, displayed anti-cancerous activity on all melanoma cells tested,Expand
Metastatic Melanoma: Insights Into the Evolution of the Treatments and Future Challenges
Melanoma is the deadliest form of skin cancer. While associated survival prognosis is good when diagnosed early, it dramatically drops when melanoma progresses into its metastatic form. Prior toExpand
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
A fluorescent immunochromatographic test using immunoliposomes for detecting microcystins and nodularins
Microcystins (MCs), a group of cyclic heptapeptides produced by common cyanobacteria (blue green algae), cause both acute and chronic toxicity. Due to their toxicity, constant monitoring in drinkingExpand
Structure activity relationship and optimization of N-(3-(2-aminothiazol-4-yl)aryl)benzenesulfonamides as anti-cancer compounds against sensitive and resistant cells.
We recently described a new family of bioactive molecules with interesting anti-cancer activities: the N-(4-(3-aminophenyl)thiazol-2-yl)acetamides. The lead compound of the series (1) displaysExpand
New Huprine Derivatives Functionalized at Position 9 as Highly Potent Acetylcholinesterase Inhibitors
A series of 24 huprine derivatives diversely functionalized at position 9 have been synthesized and evaluated for their inhibitory activity against human recombinant acetylcholinesterase (AChE).Expand