133728-25-3Relevant articles and documents
De-novo designed β-lysine derivatives can both augment and diminish the proliferation rates of E. coli through the action of Elongation Factor P
Connon, Stephen J.,Ghanim, Magda,Kelly, Vincent P.,McDonnell, Ciara M.,Mike Southern, J.
supporting information, (2022/01/24)
An investigation into the effect of modified β-lysines on the growth rates of eubacterial cells is reported. It is shown that the effects observed are due to the post translational modification of Elongation Factor P (EFP) with these compounds catalysed b
BIFUNCTIONAL COMPOUNDS AS CDK MODULATORS
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Paragraph 0333-0334, (2020/02/16)
The present application provides compounds of formulae I and II that modulate CDK protein function. Methods of making the compounds, compositions containing the compounds, and the compounds for use in a method of treating or ameliorating of diseases, disorders, or conditions associated with CDK proteins, are also disclosed.
BICYCLIC AND TRICYCLIC CAP BEARING MERCAPTOACETAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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Paragraph 0190; 0191, (2017/04/11)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
Thiol-based potent and selective HDAC6 inhibitors promote tubulin acetylation and T-regulatory cell suppressive function
Segretti, Mariana C. F.,Vallerini, Gian Paolo,Brochier, Camille,Langley, Brett,Wang, Liqing,Hancock, Wayne W.,Kozikowski, Alan P.
supporting information, p. 1156 - 1161 (2015/11/25)
Several new mercaptoacetamides were synthesized and studied as HDAC6 inhibitors. One compound, 2b, bearing an aminoquinoline cap group, was found to show 1.3 nM potency at HDAC6, with >3000-fold selectivity over HDAC1. 2b also showed excellent efficacy at increasing tubulin acetylation in rat primary cortical cultures, inducing a 10-fold increase in acetylated tubulin at 1 μM. To assess possible therapeutic effects, compounds were assayed for their ability to increase T-regulatory (Treg) suppressive function. Some but not all of the compounds increased Treg function, and thereby decreased conventional T cell activation and proliferation in vitro.
95. Design and Synthesis of Potent Macrocyclic Benzolactam Growth Hormone Secretagogues
DeVita, Robert J.,Frontier, Alison J.,Schoen, William R.,Wyvratt, Matthew J.,Fisher, Michael H.,Cheng, Kang,Chan, Wanda W.-S.,Butler, Bridget S.,Smith, Roy G.
, p. 1244 - 1259 (2007/10/03)
The synthesis of a variety of potent macrocyclic growth hormone secretagogues, i.e. 5, 9, 12, and 20-22, based on the known lead structure L-692,429 (1) is described. These conformationally constrained growth hormone secretagogues were prepared by joining
