scholarly journals Exploring the role of the α-carboxyphosphonate moiety in the HIV-RT activity of α-carboxy nucleoside phosphonates

2016 ◽  
Vol 14 (8) ◽  
pp. 2454-2465 ◽  
Author(s):  
Nicholas D. Mullins ◽  
Nuala M. Maguire ◽  
Alan Ford ◽  
Kalyan Das ◽  
Eddy Arnold ◽  
...  
Keyword(s):  
Acid Moiety ◽  
Phosphonoacetic Acid ◽  
Hiv Rt

The importance of the α-carboxy phosphonoacetic acid moiety to achieve RT inhibition, without the need for prior phosphorylation, is confirmed.

scholarly journals Acrylamide Formation in Food: A Mechanistic Perspective

2005 ◽  
Vol 88 (1) ◽  
pp. 262-267 ◽  
Author(s):  
Varoujan A Yaylayan ◽  
Richard H Stadler
Keyword(s):  
Amino Acid ◽  
Carbonyl Compounds ◽  
Azomethine Ylide ◽  
Significant Progress ◽  
Acid Moiety ◽  
Sugar Moiety ◽  
Acrylamide Formation ◽  
Amino Acid Moiety ◽  
Strecker Aldehyde

Abstract Earliest reports on the origin of acrylamide in food have confirmed asparagine as the main amino acid responsible for its formation. Available evidence suggests that sugars and other carbonyl compounds play a specific role in the decarboxylation process of asparagine, a necessary step in the generation of acrylamide. It has been proposed that Schiff base intermediate formed between asparagine and the sugar provides a low energy alternative to the decarboxylation from the intact Amadori product through generation and decomposition of oxazolidin-5-one intermediate, leading to the formation of a relatively stable azomethine ylide. Literature data indicate the propensity of such protonated ylides to undergo irreversible 1,2-prototropic shift and produce, in this case, decarboxylated Schiff bases which can easily rearrange into E Decarboxylated Amadori products can either undergo the well known β-elimination process initiated by the sugar moiety to produce 3-aminopropanamide and 1-deoxyglucosone or undergo 1,2-elimination initiated by the amino acid moiety to directly generate acrylamide. On the other hand, the Schiff intermediate can either hydrolyze and release 3-aminopropanamide or similarly undergo amino acid initiated 1,2-elimination to directly form acrylamide. Other thermolytic pathways to acrylamide—considered marginal at this stage—via the Strecker aldehyde, acrolein, and acrylic acid, are also addressed. Despite significant progress in the understanding of the mechanistic aspects of acrylamide formation, concrete evidence for the role of the different proposed intermediates in foods is still lacking.

ChemInform Abstract: The Squalestatins: Potent Inhibitors of Squalene Synthase. The Role of the Tricarboxylic Acid Moiety.

ChemInform ◽  
2010 ◽  
Vol 25 (27) ◽  
pp. no-no
Author(s):  
N. S. WATSON ◽  
R. BELL ◽  
C. CHAN ◽  
B. COX ◽  
J. L. HUTSON ◽  
...  
Keyword(s):  
Tricarboxylic Acid ◽  
Squalene Synthase ◽  
Acid Moiety

The squalestatins: potent inhibitors of squalene synthase. The role of the tricarboxylic acid moiety.

1993 ◽  
Vol 3 (12) ◽  
pp. 2541-2546 ◽  
Author(s):  
Nigel S. Watson ◽  
Richard Bell ◽  
Chuen Chan ◽  
Brian Cox ◽  
Julie L. Hutson ◽  
...  
Keyword(s):  
Tricarboxylic Acid ◽  
Squalene Synthase ◽  
Acid Moiety

scholarly journals Structure-guided design fine-tunes pharmacokinetics, tolerability, and antitumor profile of multispecific frizzled antibodies

2019 ◽  
Vol 116 (14) ◽  
pp. 6812-6817 ◽  
Author(s):  
Swetha Raman ◽  
Melissa Beilschmidt ◽  
Minh To ◽  
Kevin Lin ◽  
Francine Lui ◽  
...  
Keyword(s):  
Pancreatic Tumor ◽  
Xenograft Model ◽  
Tumor Xenograft ◽  
Acid Moiety ◽  
Plasma Exposure ◽  
Stem Cell Maintenance ◽  
Exposure In Vivo ◽  
Potential Therapeutics

Aberrant activation of Wnt/β-catenin signaling occurs frequently in cancer. However, therapeutic targeting of this pathway is complicated by the role of Wnt in stem cell maintenance and tissue homeostasis. Here, we evaluated antibodies blocking 6 of the 10 human Wnt/Frizzled (FZD) receptors as potential therapeutics. Crystal structures revealed a common binding site for these monoclonal antibodies (mAbs) on FZD, blocking the interaction with the Wnt palmitoleic acid moiety. However, these mAbs displayed gastrointestinal toxicity or poor plasma exposure in vivo. Structure-guided engineering was used to refine the binding of each mAb for FZD receptors, resulting in antibody variants with improved in vivo tolerability and developability. Importantly, the lead variant mAb significantly inhibited tumor growth in the HPAF-II pancreatic tumor xenograft model. Taken together, our data demonstrate that anti-FZD cancer therapeutic antibodies with broad specificity can be fine-tuned to navigate in vivo exposure and tolerability while driving therapeutic efficacy.

Pyrene-conjugated porphyrins for efficient mesoscopic solar cells: the role of the spacer

2014 ◽  
Vol 2 (41) ◽  
pp. 17495-17501 ◽  
Author(s):  
Jianfeng Lu ◽  
Shuangshuang Liu ◽  
Hao Li ◽  
Yan Shen ◽  
Jie Xu ◽  
...  
Keyword(s):  
Solar Cells ◽  
Carboxylic Acid ◽  
Power Conversion Efficiency ◽  
Conversion Efficiency ◽  
Power Conversion ◽  
Acid Moiety ◽  
Full Sunlight

Pyrene-conjugated porphyrin dyes with various π-spacers between the porphyrin chromophore and carboxylic acid moiety have been designed and synthesized in this study, showing an overall power conversion efficiency of 8.7% under full sunlight (AM 1.5G, 100 mW cm−2) irradiation.

scholarly journals Role of Equalized Electronegativity in Modeling HIV-RT Inhibitory Activity

2017 ◽  
Vol Volume-2 (Issue-1) ◽  
pp. 972-984
Author(s):  
Anita K. ◽  
Shweta Sharma ◽  
Suparna Ghosh | Ruchi Dubey Sharma ◽  
Keyword(s):  
Inhibitory Activity ◽  
Hiv Rt
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