Design, synthesis, and biological evaluation of 4-(1H-1,2,3-triazol-1-yl)benzamides as HSP90 inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular diversity"
DOI: 10.1007/s11030-022-10423-7
Abstract: Heat shock protein 90 (HSP90) is a promising anticancer drug target, which could be employed to construct HSP90 inhibitors-based drug conjugates for selective tumor therapy. Herein, a series of 4-(1H-1,2,3-triazol-1-yl)benzamides were rationally designed, synthesized as… read more here.
Keywords: synthesis biological; hsp90; design synthesis; triazol benzamides ... See more keywords
Recent update on discovery and development of Hsp90 inhibitors as senolytic agents.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.06.115
Abstract: Hsp90 chaperone is an encouraging target for the development of novel anticancer agents. The failure of Hsp90 inhibitors to get regulatory approval for the treatment of cancer is hindered due to toxicity, cost involved in… read more here.
Keywords: hsp90; recent update; hsp90 inhibitors; senolytic agents ... See more keywords
Development of a cell-based ligand-screening system for identifying Hsp90 inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemistry"
DOI: 10.1021/acs.biochem.9b00781
Abstract: Because of its critical roles in regulating cellular signal transduction, the molecular chaperone Heat-shock protein 90 (Hsp90) has become a novel therapeutic target for various diseases, including cancer, inflammation and neurological diseases. However, the lack… read more here.
Keywords: system; hsp90 inhibitors; cell based; ligand ... See more keywords
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01521
Abstract: Hsp90 is a new promising target for cancer treatment. Many inhibitors have been discovered as therapeutic agents, and some have passed Phase I and II. However, no one is approved by FDA yet. Novel and… read more here.
Keywords: hsp90; hsp90 inhibitors; high potent; chemistry ... See more keywords
Design and synthesis of fungal-selective resorcylate aminopyrazole Hsp90 inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00826
Abstract: The molecular chaperone Hsp90, essential in all eukaryotes, plays a multifaceted role in promoting survival, virulence and drug resistance across diverse pathogenic fungal species. The chaperone is also critically important, however, to the pathogen's human… read more here.
Keywords: design synthesis; fungal selective; hsp90; hsp90 inhibitors ... See more keywords
Combining Ensemble Learning with a Fragment-Based Topological Approach To Generate New Molecular Diversity in Drug Discovery: In Silico Design of Hsp90 Inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "ACS Omega"
DOI: 10.1021/acsomega.8b02419
Abstract: Machine learning methods have revolutionized modern science, providing fast and accurate solutions to multiple problems. However, they are commonly treated as “black boxes”. Therefore, in important scientific fields such as medicinal chemistry and drug discovery,… read more here.
Keywords: drug discovery; hsp90 inhibitors; ensemble learning;
Identification of HSP90 inhibitors as a novel class of senolytics
Sign Up to like & getrecommendations! Published in 2017 at "Nature Communications"
DOI: 10.1038/s41467-017-00314-z
Abstract: Aging is the main risk factor for many chronic degenerative diseases and cancer. Increased senescent cell burden in various tissues is a major contributor to aging and age-related diseases. Recently, a new class of drugs… read more here.
Keywords: new class; hsp90; age related; class ... See more keywords
HSP90 inhibitors disrupt a transient HSP90-HSF1 interaction and identify a noncanonical model of HSP90-mediated HSF1 regulation
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-25404-w
Abstract: Heat shock factor 1 (HSF1) initiates a broad transcriptional response to proteotoxic stress while also mediating a cancer-specific transcriptional program. HSF1 is thought to be regulated by molecular chaperones, including Heat Shock Protein 90 (HSP90).… read more here.
Keywords: hsp90; hsp90 inhibitors; inhibitors disrupt; hsf1 ... See more keywords
Hsp90 inhibitors enhance the antitumoral effect of osimertinib and overcome osimertinib resistance in non-small cell cell lung cancer cell models
Sign Up to like & getrecommendations! Published in 2019 at "Annals of Oncology"
DOI: 10.1093/annonc/mdz238.034
Abstract: Abstract Background The epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) osimertinib improves therapy for non-small cell lung cancer (NSCLC) patients who possess EGR mutations. However, invariable acquired resistance appears due to several molecular mechanisms.… read more here.
Keywords: hsp90 inhibitors; osimertinib resistance; oncology; non small ... See more keywords
Heat shock protein 90 inhibitors block the anti-nociceptive effects of opioids in mouse chemotherapy-induced neuropathy and cancer bone pain models.
Sign Up to like & getrecommendations! Published in 2020 at "Pain"
DOI: 10.1097/j.pain.0000000000001886
Abstract: Heat shock protein 90 (Hsp90) is a ubiquitous signal transduction regulator, and Hsp90 inhibitors are in clinical development as cancer therapeutics. However, there have been very few studies on the impact of Hsp90 inhibitors on… read more here.
Keywords: cancer; hsp90 inhibitors; pain; anti nociception ... See more keywords
Model System Identifies Kinetic Driver of Hsp90 Inhibitor Activity against African Trypanosomes and Plasmodium falciparum
Sign Up to like & getrecommendations! Published in 2018 at "Antimicrobial Agents and Chemotherapy"
DOI: 10.1128/aac.00056-18
Abstract: Hsp90 inhibitors, well studied in the laboratory and clinic for antitumor indications, have promising activity against protozoan pathogens, including Trypanosoma brucei which causes African sleeping sickness, and the malaria parasite, Plasmodium falciparum. To progress these… read more here.
Keywords: driver; system; hsp90 inhibitors; plasmodium falciparum ... See more keywords