Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114211
Abstract: A series of novel non-covalent peptidomimetic proteasome inhibitors possessing bulky group at the C-terminus and N-alkylation at the N-terminus were designed with the aim to increase metabolic stabilities in vivo. All the target compounds were screened… read more here.
Keywords: proteasome inhibitors; guided optimization; non covalent; ic50 ... See more keywords
Discovery of a Potent Thieno[2,3-d]pyrimidine-2,4-dione-Based Protoporphyrinogen IX Oxidase Inhibitor through an In Silico Structure-Guided Optimization Approach.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.1c05665
Abstract: A key objective for herbicide research is to develop new compounds with improved bioactivity. Protoporphyrinogen IX oxidase (PPO) is an essential target for herbicide discovery. Here, we report using an in silico structure-guided optimization approach… read more here.
Keywords: thieno pyrimidine; pyrimidine dione; structure guided; guided optimization ... See more keywords
Deep learning guided optimization of human antibody against SARS-CoV-2 variants with broad neutralization
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2122954119
Abstract: Significance SARS-CoV-2 continues to evolve through emerging variants, more frequently observed with higher transmissibility. Despite the wide application of vaccines and antibodies, the selection pressure on the Spike protein may lead to further evolution of… read more here.
Keywords: guided optimization; deep learning; sars cov; learning guided ... See more keywords
Contractility sensor-guided optimization of cardiac resynchronization therapy: results from the RESPOND-CRT trial
Sign Up to like & getrecommendations! Published in 2017 at "European Heart Journal"
DOI: 10.1093/eurheartj/ehw526
Abstract: Aims Although cardiac resynchronization therapy (CRT) is effective in patients with systolic heart failure (HF) and a wide QRS interval, a substantial proportion of patients remain non-responsive. The SonR contractility sensor embedded in the right… read more here.
Keywords: contractility sensor; respond crt; optimization; guided optimization ... See more keywords
Boundary-Guided Optimization Framework for Saliency Refinement
Sign Up to like & getrecommendations! Published in 2018 at "IEEE Signal Processing Letters"
DOI: 10.1109/lsp.2018.2801821
Abstract: Salient object detection has made a rapid progress in recent years. To improve the quality of initial saliency maps, existing algorithms typically refine them via a neighbor-constrained smoothing model, which assigns similar saliency values to… read more here.
Keywords: saliency; boundary guided; guided optimization; optimization ... See more keywords
Expert-guided optimization for 3D printing of soft and liquid materials
Sign Up to like & getrecommendations! Published in 2018 at "PLoS ONE"
DOI: 10.1371/journal.pone.0194890
Abstract: Additive manufacturing (AM) has rapidly emerged as a disruptive technology to build mechanical parts, enabling increased design complexity, low-cost customization and an ever-increasing range of materials. Yet these capabilities have also created an immense challenge… read more here.
Keywords: expert guided; guided optimization; optimization printing; parameter space ... See more keywords