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Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112440
Abstract: Mycobacterium tuberculosis (M.tb), the etiologic agent of tuberculosis, remains the leading cause of death from a single infectious agent worldwide. The emergence of drug-resistant M.tb strains stresses the need for drugs acting on new targets.…
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Keywords:
maba;
tuberculosis;
discovery first;
maba fabg1 ... See more keywords
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Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01768
Abstract: The first examples of threonine tyrosine kinase (TTK) PROTACs were designed and synthesized. Two of the most potent molecules, 8e and 8j, demonstrated strong TTK degradation in COLO-205 human colorectal cancer cells with DC50 values…
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Keywords:
first examples;
threonine tyrosine;
tyrosine kinase;
examples threonine ... See more keywords
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Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01774
Abstract: Regulating SOS1 functions may result in targeted pan-KRAS therapies. Small-molecule SOS1 inhibitors showed promising anticancer potential, and the most advanced inhibitor BI 1701963 is currently under phase I clinical studies. SOS1 agonists provide new opportunities…
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Keywords:
cancer;
agonist;
sos1 protacs;
discovery first ... See more keywords
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Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00263
Abstract: Indoleamine 2,3-dioxygenase 2 (IDO2), a closely related homologue of well-studied immunomodulatory enzyme IDO1, has been identified as a pathogenic mediator of inflammatory autoimmunity in preclinical models. Therapeutic targeting IDO2 in autoimmune diseases has been challenging…
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Keywords:
inhibitor;
arthritis;
ido2;
ido2 inhibitor ... See more keywords
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Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00652
Abstract: The highly homologous protein lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9), have been implicated in various human diseases. To investigate functions of G9a and GLP in…
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Keywords:
glp;
discovery first;
first class;
covalent ... See more keywords
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Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c02123
Abstract: Peroxisome proliferator-activator receptors α/δ (PPARα/δ) are considered as potential drug targets for cholestatic liver diseases (CLD) via ameliorating hepatic cholestasis, inflammation, and fibrosis. In this work, we developed a series of hydantoin derivatives as potent…
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Keywords:
ppar;
ppar dual;
liver diseases;
discovery first ... See more keywords
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Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01371
Abstract: Signal peptide peptidase-like 2a (SPPL2a) is an aspartic intramembrane protease which has recently been shown to play an important role in the development and function of antigen presenting cells such as B lymphocytes and dendritic…
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Keywords:
sppl2a;
signal peptide;
peptidase like;
discovery first ... See more keywords
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1
Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01528
Abstract: MEK1 and MEK2 (also known as MAP2K1 and MAP2K2) are the "gatekeepers" of the ERK signaling output with redundant roles in controlling ERK activity. Numerous inhibitors targeting MEK1/2 have been developed including three FDA-approved drugs.…
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Keywords:
degrader;
kinase;
discovery first;
mek1 ... See more keywords
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Published in 2018 at "JCI insight"
DOI: 10.1172/jci.insight.99208
Abstract: Soluble cytokine receptors function as decoy receptors to attenuate cytokine-mediated signaling and modulate downstream cellular responses. Dysregulated overproduction of soluble receptors can be pathological, such as soluble ST2 (sST2), a prognostic biomarker in cardiovascular diseases,…
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Keywords:
vivo;
st2 inhibitors;
discovery first;
proteomics discovery ... See more keywords
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Published in 2021 at "Molecules"
DOI: 10.3390/molecules26247483
Abstract: Ribosomally synthesized and post-translationally modified peptides (RiPPs) are a structurally diverse group of natural products. They feature a wide range of intriguing post-translational modifications, as exemplified by the biarylitides. These are a family of cyclic…
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Keywords:
guided discovery;
myxarylin;
biarylitide;
biaryl ... See more keywords