Publications associées à Anticholinestérase

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Henning Paul-Julius Stahlberg, Dongchun Ni

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In previously reported structures, the reaction cycle was halted by the absence of substrates or ATP, mutation of catalytic residue ...

NATURE RESEARCH2021

Rivastigmine decreases brain damage in HIV patients with mild cognitive deficits

David Paul Roger Romascano, Reto Meuli, Alessandro Daducci, Cristina Granziera, Djalel Eddine Meskaldji, Guillaume Bonnier, Ruslan Aydarkhanov, François Lazeyras

Rivastigmine has been shown to improve cognition in HIV+ patients with minor neurocognitive disorders; however, the mechanisms underlying such beneficial effect are currently unknown. To assess whether rivastigmine therapy is associated with decreased brai ...

Wiley2017

Acidic tumor microenvironment abrogates the efficacy of mTORC1 inhibitors

Anne Planche, Tania Santoro

Background: Blocking the mechanistic target of rapamycin complex-1 (mTORC1) with chemical inhibitors such as rapamycin has shown limited clinical efficacy in cancer. The tumor microenvironment is characterized by an acidic pH which interferes with cancer t ...

Biomed Central Ltd2016

1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)

Pierre Vogel, George Coukos, Somi Reddy Majjigapu, Olivier Michielin

Indoleamine 2,3-dioxygenase 2 (IDO2) is a potential therapeutic target for the treatment of diseases that involve immune escape such as cancer. In contrast to IDO1, only a very limited number of inhibitors have been described for IDO2 due to inherent diffi ...

Pergamon-Elsevier Science Ltd2016

Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides

Christian Heinis, Rudolf Hovius, Florence Pojer, Shiyu Chen, Ranganath Gopalakrishnan

The disulfide bonds that form between two cysteine residues are important in defining and rigidifying the structures of proteins and peptides. In polypeptides containing multiple cysteine residues, disulfide isomerization can lead to multiple products with ...

Nature Publishing Group2014

The Growing Arsenal of ATP-Competitive and Allosteric Inhibitors of BCR-ABL

Oliver Hantschel

The BCR-ABL fusion kinase is the driving mutation of chronic myelogenous leukemias and is also expressed in a subset of acute lymphoblastic leukemias. Recent advances in elucidating the structure, regulation, and signaling of BCR-ABL have led to the identi ...

Amer Assoc Cancer Research2012

Automated design of ligands to polypharmacological profiles

Daniel Constam

The clinical efficacy and safety of a drug is determined by its activity profile across many proteins in the proteome. However, designing drugs with a specific multi-target profile is both complex and difficult. Therefore methods to design drugs rationally ...

Nature Publishing Group2012

Structure and function of the transketolase from Mycobacterium tuberculosis and comparison with the human enzyme

Stewart Cole, Florence Pojer, Elizabeth Fullam

The transketolase (TKT) enzyme in Mycobacterium tuberculosis represents a novel drug target for tuberculosis treatment and has low homology with the orthologous human enzyme. Here, we report on the structural and kinetic characterization of the transketola ...

Royal Soc2012

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Anticholinestérase

Tracking spatiotemporal localisation and interactions of the innate immune sensor STING

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Rivastigmine decreases brain damage in HIV patients with mild cognitive deficits

Acidic tumor microenvironment abrogates the efficacy of mTORC1 inhibitors

1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)

Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides

The Growing Arsenal of ATP-Competitive and Allosteric Inhibitors of BCR-ABL

Automated design of ligands to polypharmacological profiles

Structure and function of the transketolase from Mycobacterium tuberculosis and comparison with the human enzyme

Structure, regulation, signaling, and targeting of abl kinases in cancer

Graph Chatbot

Chattez avec Graph Search

Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism

Tracking spatiotemporal localisation and interactions of the innate immune sensor STING

The Growing Arsenal of ATP-Competitive and Allosteric Inhibitors of BCR-ABL

Structure, regulation, signaling, and targeting of abl kinases in cancer

Rivastigmine decreases brain damage in HIV patients with mild cognitive deficits

Dithiol amino acids can structurally shape and enhance the ligand-binding properties of polypeptides

Acidic tumor microenvironment abrogates the efficacy of mTORC1 inhibitors

Automated design of ligands to polypharmacological profiles

1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)

Structure and function of the transketolase from Mycobacterium tuberculosis and comparison with the human enzyme