Genie in a bottle: controlled release helps tame natural polypharmacology?
Sign Up to like & getrecommendations! Published in 2019 at "Current opinion in chemical biology"
DOI: 10.1016/j.cbpa.2019.02.014
Abstract: Ability to faithfully report drug-target interactions constitutes a major critical parameter in preclinical/clinical settings. Yet the assessment of target engagement remains challenging, particularly for promiscuous and/or polypharmacologic ligands. Drawing from our improved insights into native… read more here.
Keywords: helps tame; bottle controlled; controlled release; polypharmacology ... See more keywords
Polypharmacology Approaches against the Pseudomonas aeruginosa MvfR Regulon and Their Application in Blocking Virulence and Antibiotic Tolerance.
Sign Up to like & getrecommendations! Published in 2017 at "ACS chemical biology"
DOI: 10.1021/acschembio.6b01139
Abstract: Pseudomonas aeruginosa is an important nosocomial pathogen that is frequently recalcitrant to available antibiotics, underlining the urgent need for alternative therapeutic options against this pathogen. Targeting virulence functions is a promising alternative strategy as it… read more here.
Keywords: mvfr; pseudomonas aeruginosa; polypharmacology; mvfr regulon ... See more keywords
Privileged Structures and Polypharmacology within and between Protein Families
Sign Up to like & getrecommendations! Published in 2018 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.8b00364
Abstract: Polypharmacology is often a key contributor to the efficacy of a drug, but is also a potential risk. We investigated two hits discovered via a cell-based phenotypic screen, the CDK9 inhibitor CCT250006 (1) and the… read more here.
Keywords: protein families; privileged structures; polypharmacology; polypharmacology within ... See more keywords
Polypharmacology in the treatment of Chagas disease.
Sign Up to like & getrecommendations! Published in 2018 at "Current medicinal chemistry"
DOI: 10.2174/0929867325666180410101728
Abstract: The current treatment of Chagas disease is based on monopharmacology where the used drugs have limited efficacy and severe side effects. In order to overcome these limitations some tools have been described including development or… read more here.
Keywords: polypharmacology; treatment; chagas; treatment chagas ... See more keywords
From Combinations to Single-Molecule Polypharmacology—Cromolyn-Ibuprofen Conjugates for Alzheimer’s Disease
Sign Up to like & getrecommendations! Published in 2021 at "Molecules"
DOI: 10.3390/molecules26041112
Abstract: Despite Alzheimer’s disease (AD) incidence being projected to increase worldwide, the drugs currently on the market can only mitigate symptoms. Considering the failures of the classical paradigm “one target-one drug-one disease” in delivering effective medications… read more here.
Keywords: single molecule; polypharmacology; alzheimer disease; disease ... See more keywords