Polymerase assays for lead discovery: An overall review of methodologies and approaches.
Sign Up to like & getrecommendations! Published in 2018 at "Analytical biochemistry"
DOI: 10.1016/j.ab.2018.09.022
Abstract: Polymerases represent an attractive molecular target for antibacterial drug development, antiviral intervention and cancer therapy. Over the past decade, academic groups and scientists from pharmaceutical industry have developed a large plethora of different functional assays… read more here.
Keywords: assays lead; discovery overall; review; polymerase assays ... See more keywords
Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01563
Abstract: G-quadruplex stabilizers are an established opportunity in anticancer chemotherapy. To circumvent the antiproliferative effects of G4 ligands, cancer cells recruit PARP enzymes at telomeres. Herein, starting from the structural similarity of a potent G4 ligand… read more here.
Keywords: dual quadruplex; discovery dual; stabilizers poly; quadruplex stabilizers ... See more keywords
Using Fragment-Based Approaches to Discover New Antibiotics
Sign Up to like & getrecommendations! Published in 2018 at "Slas Discovery"
DOI: 10.1177/2472555218773034
Abstract: Fragment-based lead discovery has emerged over the past two decades as a successful approach to generate novel lead candidates in drug discovery programs. The two main advantages over conventional high-throughput screening (HTS) are more efficient… read more here.
Keywords: based approaches; new antibiotics; lead discovery; fragment based ... See more keywords
Crystal polymorphism in fragment-based lead discovery of ligands of the catalytic domain of UGGT, the glycoprotein folding quality control checkpoint
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Molecular Biosciences"
DOI: 10.3389/fmolb.2022.960248
Abstract: None of the current data processing pipelines for X-ray crystallography fragment-based lead discovery (FBLD) consults all the information available when deciding on the lattice and symmetry (i.e., the polymorph) of each soaked crystal. Often, X-ray… read more here.
Keywords: fragment based; lead discovery; catalytic domain; based lead ... See more keywords