204919-57-3Relevant academic research and scientific papers
Increased polymer length of oligopeptide-substituted polynorbornenes with LiCl
Roberts, Kenny S.,Sampson, Nicole S.
, p. 2020 - 2023 (2003)
The ring-opening metathesis polymerization (ROMP) reaction is extraordinarily useful for the preparation of a large variety of polymers. We report that the length (n = 25-50) of high-substituent-density oligopeptide polymers synthesized by ROMP is dramati
Optimization and anti-cancer properties of fluoromethylketones as covalent inhibitors for ubiquitin C-terminal hydrolase L1
Chen, Hao,Das, Chittaranjan,Flaherty, Daniel P.,Galardy, Paul J.,Hewitt, Chad S.,Hussain, Sajjad,Imhoff, Ryan D.,Krabill, Aaron D.,Muli, Christine S.,Wendt, Michael K.
, (2021/05/31)
The deubiquitinating enzyme (DUB) UCHL1 is implicated in various disease states including neurodegenerative disease and cancer. However, there is a lack of quality probe molecules to gain a better understanding on UCHL1 biology. To this end a study was carried out to fully characterize and optimize the irreversible covalent UCHL1 inhibitor VAEFMK. Structure-activity relationship studies identified modifications to improve activity versus the target and a full cellular characterization was carried out for the first time with this scaffold. The studies produced a new inhibitor, 34, with an IC50 value of 7.7 μM against UCHL1 and no observable activity versus the closest related DUB UCHL3. The molecule was also capable of selectively inhibiting UCHL1 in cells and did not demonstrate any discernible off-target toxicity. Finally, the molecule was used for initial probe studies to assess the role of UCHL1 role in proliferation of myeloma cells and migration behavior in small cell lung cancer cells making 34 a new tool to be used in the biological evaluation of UCHL1.
A facile synthetic method to prepare fluorescently labeled ROMP polymers
Roberts, Kenny S.,Sampson, Nicole S.
, p. 3253 - 3255 (2007/10/03)
(Chemical Equation Presented) To probe the activities of sperm ADAM protein (fertilinβ), we devised a general synthetic strategy to generate fluorescently labeled fertilinβ oligopeptide polymers. Immunofluorescence studies with these polymers demonstrated that fertilinβ polymers bind specifically to a protein receptor on the mouse egg plasma membrane.
(Substituted)acyl dipeptidyl inhibitors of the ICE/ced-3 family of cysteine proteases
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Page 20-21, (2010/02/05)
This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of pa
