The 1.8 Å Crystal Structure of ACTIBIND Suggests a Mode of Action for T2 Ribonucleases As Antitumorigenic Agents

2012 ◽  
Vol 55 (3) ◽  
pp. 1013-1020 ◽  
Author(s):  
Marina de Leeuw ◽  
Ana González ◽  
Assaf Lanir ◽  
Levava Roiz ◽  
Patricia Smirnoff ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Mode Of Action

scholarly journals AFN-1252 is a potent inhibitor of enoyl-ACP reductase from B urkholderia pseudomallei -Crystal structure, mode of action, and biological activity

2015 ◽  
Vol 24 (5) ◽  
pp. 832-840 ◽  
Author(s):  
Krishnamurthy Narasimha Rao ◽  
Anirudha Lakshminarasimhan ◽  
Sarah Joseph ◽  
Swathi U. Lekshmi ◽  
Ming-Seong Lau ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Biological Activity ◽  
Mode Of Action ◽  
Potent Inhibitor ◽  
Enoyl Acp Reductase

scholarly journals The Crystal Structure and Mode of Action of Trans-Sialidase, a Key Enzyme in Trypanosoma cruzi Pathogenesis

2002 ◽  
Vol 10 (4) ◽  
pp. 757-768 ◽  
Author(s):  
Alejandro Buschiazzo ◽  
Marı́a F. Amaya ◽  
Marı́a L. Cremona ◽  
Alberto C. Frasch ◽  
Pedro M. Alzari
Keyword(s):  
Crystal Structure ◽  
Trypanosoma Cruzi ◽  
Mode Of Action ◽  
Key Enzyme

scholarly journals The Crystal Structure of Human Transketolase and New Insights into Its Mode of Action

2010 ◽  
Vol 285 (41) ◽  
pp. 31559-31570 ◽  
Author(s):  
Lars Mitschke ◽  
Christoph Parthier ◽  
Kathrin Schröder-Tittmann ◽  
Johannes Coy ◽  
Stefan Lüdtke ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Mode Of Action

scholarly journals Crystal structure of Arabidopsis thaliana HPPK/DHPS, a bifunctional enzyme and target of the herbicide asulam

2021 ◽  
Author(s):  
Grishma Vadlamani ◽  
Kirill V Sukhoverkov ◽  
Joel Haywood ◽  
Karen J Breese ◽  
Mark F Fisher ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Arabidopsis Thaliana ◽  
Mode Of Action ◽  
Rational Design ◽  
Binding Pocket ◽  
Structural Basis ◽  
Metabolic Resistance ◽  
Folate Biosynthesis ◽  
Limited Opportunity ◽  
Regulatory Scrutiny

Herbicides are vital for modern agriculture, but their utility is threatened by genetic or metabolic resistance in weeds as well as heightened regulatory scrutiny. Of the known herbicide modes of action, 6-hydroxymethyl-7,8-dihydropterin synthase (DHPS) which is involved in folate biosynthesis, is targeted by just one commercial herbicide, asulam. A mimic of the substrate para-aminobenzoic acid, asulam is chemically similar to sulfonamide antibiotics - and while still in widespread use, asulam has faced regulatory scrutiny. With an entire mode of action represented by just one commercial agrochemical, we sought to improve the understanding of its plant target. Here we solve a 2.6 Å resolution crystal structure for Arabidopsis thaliana DHPS that is conjoined to 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase (HPPK) and reveal a strong structural conservation with bacterial counterparts at the sulfonamide-binding pocket of DHPS. We demonstrate asulam and the antibiotics sulfacetamide and sulfamethoxazole have herbicidal as well as antibacterial activity and explore the structural basis of their potency by modelling these compounds in mitochondrial HPPK/DHPS. Our findings suggest limited opportunity for the rational design of plant selectivity from asulam and that pharmacokinetic or delivery differences between plants and microbes might be the best approaches to safeguard this mode of action.

Crystal structure and mode of action of a class V chitinase from Nicotiana tabacum

2011 ◽  
Vol 75 (3) ◽  
pp. 291-304 ◽  
Author(s):  
Takayuki Ohnuma ◽  
Tomoyuki Numata ◽  
Takuo Osawa ◽  
Mamiko Mizuhara ◽  
Kjell M. Vårum ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Nicotiana Tabacum ◽  
Mode Of Action ◽  
Class V

Crystal structure and electrostatic properties of prednisolone acetate studied using a transferred multipolar atom model

2017 ◽  
Vol 73 (6) ◽  
pp. 430-436
Author(s):  
Ammara Shahid ◽  
Sajida Noureen ◽  
Muhammad Iqbal Choudhary ◽  
Sammer Yousuf ◽  
Maqsood Ahmed
Keyword(s):  
Crystal Structure ◽  
Electron Density ◽  
Mode Of Action ◽  
Prednisolone Acetate ◽  
Drug Molecule ◽  
Electrostatic Properties ◽  
Atom Model ◽  
Derived Properties ◽  
Ophthalmic Drug

Prednisolone acetate {systematic name: 2-[(8S,9S,10R,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl acetate}, is an ophthalmic drug that belongs to the class of corticosteroids. Its crystal structure was refined using the classical independent atom model (IAM) and a transferred multipolar atom model using the ELMAM2 database. The results of both refinements have been compared. The ELMAM2 refinement was found to be superior in terms of the refinement statistics. It has been shown that certain electron-density-derived properties can be calculated on the basis of the transferred parameters for crystals which diffract to ordinary resolution. The procedure proves helpful in understanding the mode of action of the drug molecule.

scholarly journals Dirigent Protein Mode of Action Revealed by the Crystal Structure of AtDIR6

2016 ◽  
Vol 172 (4) ◽  
pp. 2165-2175 ◽  
Author(s):  
Raphael Gasper ◽  
Isabelle Effenberger ◽  
Piotr Kolesinski ◽  
Barbara Terlecka ◽  
Eckhard Hofmann ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Mode Of Action ◽  
Dirigent Protein
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