134019-73-1Relevant articles and documents
Solid-phase synthesis of peptidosulfonamide containing peptides derived from Leu-enkephalin
De Bont, Dries B.A.,Dijkstra, Gerard D.H.,Den Hartog, Jack A.J.,Liskamp, Rob M.J.
, p. 3035 - 3040 (1996)
Using Boc or Fmoc-protected β-substituted aminoethanesulfonyl chlorides (2-substituted taurylchlorides) the solid-phase synthesis of dipeptidosulfonamides as well as peptidosulfonamide containing peptides derived from Leu-enkephalin is described. The binding activity of the peptidosulfonamide YGGFL derivatives is reported.
Design, synthesis and photochemical reactivation of caged prodrugs of 8-hydroxyquinoline-based enzyme inhibitors
Ariyasu, Shinya,Mizuseda, Yuki,Hanaya, Kengo,Aoki, Shin
, p. 642 - 648 (2014)
8-Hydroxyquinoline (HQ)-based compounds have recently been proposed as potential candidates for drugs for treating human immunodeficiency virus (HIV), cancer, neurodegenerative diseases (Alzheimer's and Parkinson's disease), and parasitic and bacterial infections. However, HQ itself and its derivatives might be toxic due to their intrinsic affinity for metal cations in living systems. One possible strategy for suppressing the toxicity and side effects of drugs with metal chelation properties, such as HQ, would be masking the critically important moieties with protecting groups that can be subsequently removed under specific conditions. In our previous work, we reported that HQ analogs are potent and selective inhibitors (Kivalues=0.16-29 μM) of aminopeptidase from Aeromonas proteolytica (AAP) (EC 3.4.11.10), a dinuclear Zn2+ peptidase. Based on this background information, HQ sulfonates were synthesized as prodrugs of HQ-based AAP-inhibitors that can be reactivated by photochemical cleavage of the S-O bond in the sulfonate groups. The findings indicate that HQ sulfonates containing methanesulfonyl and 2-aminoethanesulfonyl groups are essentially stable under physiological conditions and undergo photolysis to regenerate the corresponding HQ compounds that function as AAP inhibitors. This methodology could be applied to the design of similar types of Zn2+ hydrolase inhibitors and prodrugs.
Helical Antimicrobial Sulfono-γ-AApeptides
Li, Yaqiong,Wu, Haifan,Teng, Peng,Bai, Ge,Lin, Xiaoyang,Zuo, Xiaobing,Cao, Chuanhai,Cai, Jianfeng
, p. 4802 - 4811 (2015)
Host-defense peptides (HDPs) such as magainin 2 have emerged as potential therapeutic agents combating antibiotic resistance. Inspired by their structures and mechanism of action, herein we report the first example of antimicrobial helical sulfono-γ-AApeptide foldamers. The lead molecule displays broad-spectrum and potent antimicrobial activity against multi-drug-resistant Gram-positive and Gram-negative bacterial pathogens. Time-kill studies and fluorescence microscopy suggest that sulfono-γ-AApeptides eradicate bacteria by taking a mode of action analogous to that of HDPs. Clear structure-function relationships exist in the studied sequences. Longer sequences, presumably adopting more-defined helical structures, are more potent than shorter ones. Interestingly, the sequence with less helical propensity in solution could be more selective than the stronger helix-forming sequences. Moreover, this class of antimicrobial agents are resistant to proteolytic degradation. These results may lead to the development of a new class of antimicrobial foldamers combating emerging antibiotic-resistant pathogens.
METHODS FOR DELAYING, PREVENTING, AND TREATING ACQUIRED RESISTANCE TO RAS INHIBITORS
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, (2022/01/04)
The present disclosure relates to compositions and methods for the treatment of diseases or disorders (e.g., cancer) with bi-steric inhibitors of mTOR in combination with RAS inhibitors. Specifically, in some embodiments this disclosure includes compositions and methods for inducing apoptosis of tumor cells and/or for delaying, preventing, or treating acquired resistance to RAS inhibitors using bi-steric mTOR inhibitors.
COMPOUNDS AND USES THEREOF
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, (2020/08/22)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
TETRAZINES FOR HIGH CLICK RELEASE SPEED AND YIELD
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Page/Page column 232; 235, (2021/01/22)
Disclosed herein are tetrazines substituted with groups that result in a high click conjugation yield and high click release yields. In some of several other aspects, the invention relates to combinations and kits comprising said tetrazines and a dienophile, preferably a trans-cyclooctene. In another aspect, the compounds, combinations, and kits are for use as a medicament.
C26-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
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, (2019/11/21)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
C40-, C28-, AND C-32-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
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, (2019/11/19)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
INHIBITORS OF LYSINE BIOSYNTHESIS VIA THE DIAMINOPIMELATE PATHWAY
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, (2020/01/24)
The present invention relates to compounds that have the ability to inhibit lysine biosynthesis via the diaminopimelate pathway in certain organisms. As a result of this activity these compounds can be used in applications where inhibition of lysine biosynthesis is useful. Applications of this type include the use of the compound as herbicides and/or anti-bacterial agents.
SUBSTITUTED SULFONYL HYDRAZIDES AS INHIBITORS OF LYSINE BIOSYNTHESIS VIA THE DIAMINOPIMELATE PATHWAY
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, (2020/01/24)
The present invention relates to substituted sulfonyl hydrazides that have the ability to inhibit lysine biosynthesis via the diaminopimelate pathway in certain organisms. As a result of this activity these compounds can be used in applications where inhibition of lysine biosynthesis is useful applications of this type include the use of the compound as herbicides and/or anti- bacterial agents.
