Allosteric small molecule modulators of nuclear receptors
Sign Up to like & getrecommendations! Published in 2019 at "Molecular and Cellular Endocrinology"
DOI: 10.1016/j.mce.2019.01.022
Abstract: Nuclear Receptors (NRs) are multi-domain proteins, whose natural regulation occurs via ligands for a classical, orthosteric, binding pocket and via intra- and inter-domain allosteric mechanisms. Allosteric modulation of NRs via synthetic small molecules has recently… read more here.
Keywords: nuclear receptors; small molecule; small molecules; molecule modulators ... See more keywords
Screen for Small-Molecule Modulators of Circadian Rhythms Reveals Phenazine as a Redox-State Modifying Clockwork Tuner.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00240
Abstract: A high-throughput cell-based screen identified redox-active small molecules that produce a period lengthening of the circadian rhythm. The strongest period lengthening phenotype was induced by a phenazine carboxamide (VU661). Comparison to two isomeric benzquinoline carboxamides… read more here.
Keywords: small molecule; state; screen; molecule modulators ... See more keywords
Tuning the rate of aggregation of hIAPP into amyloid using small-molecule modulators of assembly
Sign Up to like & getrecommendations! Published in 2022 at "Nature Communications"
DOI: 10.1038/s41467-022-28660-7
Abstract: Human islet amyloid polypeptide (hIAPP) self-assembles into amyloid fibrils which deposit in pancreatic islets of type 2 diabetes (T2D) patients. Here, we applied chemical kinetics to study the mechanism of amyloid assembly of wild-type hIAPP… read more here.
Keywords: small molecule; hiapp; aggregation; aggregation hiapp ... See more keywords
Small molecule modulators of IL-17A/IL-17RA: a patent review (2013-2021)
Sign Up to like & getrecommendations! Published in 2022 at "Expert Opinion on Therapeutic Patents"
DOI: 10.1080/13543776.2022.2143264
Abstract: ABSTRACT Introduction Interleukin-17A (IL-17A) is a well-established pro-inflammatory cytokine, which plays a pivotal role in immune and autoimmune diseases including psoriasis, asthma, psoriatic arthritis, and rheumatoid arthritis. Three currently approved monoclonal antibodies (mAbs) are in… read more here.
Keywords: small molecule; molecule modulators; molecule; 17a 17ra ... See more keywords
Synthetic Small Molecule Modulators of Hsp70 and Hsp40 Chaperones as Promising Anticancer Agents
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24044083
Abstract: A class of chaperones dubbed heat shock protein 70 (Hsp70) possesses high relevance in cancer diseases due to its cooperative activity with the well-established anticancer target Hsp90. However, Hsp70 is closely connected with a smaller… read more here.
Keywords: small molecule; molecule modulators; synthetic small; hsp70 hsp40 ... See more keywords