A structure-activity relationship study of small-molecule inhibitors of GLI1-mediated transcription

Biopolymers ◽  
2010 ◽  
Vol 95 (1) ◽  
pp. 24-30 ◽  
Author(s):  
Marcelo Actis ◽  
Michele C. Connelly ◽  
Anand Mayasundari ◽  
Chandanamali Punchihewa ◽  
Naoaki Fujii
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study

scholarly journals Discovery and Structure Activity Relationship of Small Molecule Inhibitors of Toxic β-Amyloid-42 Fibril Formation

2012 ◽  
Vol 287 (41) ◽  
pp. 34786-34800 ◽  
Author(s):  
Heiko Kroth ◽  
Annalisa Ansaloni ◽  
Yvan Varisco ◽  
Asad Jan ◽  
Nampally Sreenivasachary ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Structure Activity Relationship ◽  
Fibril Formation ◽  
Activity Relationship ◽  
Structure Activity ◽  
Β Amyloid ◽  
Relationship Of

scholarly journals Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1)

MedChemComm ◽  
2016 ◽  
Vol 7 (9) ◽  
pp. 1793-1796 ◽  
Author(s):  
H. Ü. Kaniskan ◽  
M. S. Eram ◽  
J. Liu ◽  
D. Smil ◽  
M. L. Martini ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
High Potency ◽  
Arginine Methyltransferase ◽  
Design And Synthesis ◽  
Structure Activity ◽  
Methyltransferase 1

Structure–activity relationship studies, starting from a fragment hit, resulted in discovery of the compound 9, an inhibitor of CARM1 with high potency and selectivity.

Identification and Structure-Activity Relationship Studies of Small-Molecule Inhibitors of the Methyllysine Reader Protein Spindlin1

ChemMedChem ◽  
2016 ◽  
Vol 11 (20) ◽  
pp. 2327-2338 ◽  
Author(s):  
Dina Robaa ◽  
Tobias Wagner ◽  
Chiara Luise ◽  
Luca Carlino ◽  
Joel McMillan ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Structure–Activity Relationship for Small Molecule Inhibitors of Nicotinamide N-Methyltransferase

2017 ◽  
Vol 60 (12) ◽  
pp. 5015-5028 ◽  
Author(s):  
Harshini Neelakantan ◽  
Hua-Yu Wang ◽  
Virginia Vance ◽  
Jonathan D. Hommel ◽  
Stanton F. McHardy ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

scholarly journals A unique small molecule pair controls the plant circadian clock

2020 ◽  
Author(s):  
Takahiro N Uehara ◽  
Saori Takao ◽  
Hiromi Matsuo ◽  
Ami N. Saito ◽  
Eisuke Ota ◽  
...  
Keyword(s):  
Circadian Clock ◽  
Small Molecule ◽  
Molecular Mechanisms ◽  
Response Regulator ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Genetic Redundancy ◽  
Chemical Library ◽  
Structure Activity ◽  
Relationship Study

SummaryCircadian clocks are the biological time keeping systems that coordinate genetic, metabolic, and physiological behaviors with the external day-night cycle. Previous studies have suggested possible molecular mechanisms for the circadian clock in Arabidopsis thaliana (Arabidopsis), but there might be additional mechanisms that have been hidden due to genetic redundancy.A clock reporter line of Arabidopsis was screened against the 10,000 chemicals in the Maybridge Hitfinder10K chemical library, and a structure-activity relationship study of hit compounds was conducted. Clock mutants were treated with two of the small molecules to gain insight into their mode of action.The screening identified 5-(3,4-dichlorophenyl)-1-phenyl-1,7-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4,6(5H)-dione (TU-892) as a period lengthening molecule. From a structure-activity relationship study, we found that a molecule possessing 2,4-dichlorophenyl instead of a 3,4-dichlorophenyl group (TU-923) had period shortening activity. The period shortening activity of TU-923 was reversed to a lengthening activity in double mutants lacking PSEUDO-RESPONSE REGULATOR 9 (PRR9) and PRR7 (prr9-10 prr7-11).Our study provides a unique small molecule pair that regulates the pace of the clock in opposite ways, likely by targeting unknown factors. Small differences at the atomic level can reverse the period tuning activities. PRR9 and PRR7 are essential for the activity of TU-923 in period shortening.

Identification and structure-activity relationship studies of small molecule inhibitors of the human cathepsin D

2021 ◽  
Vol 29 ◽  
pp. 115879
Author(s):  
Sandeep Goyal ◽  
Ketul V. Patel ◽  
Yadav Nagare ◽  
Digambar B. Raykar ◽  
Santosh S. Raikar ◽  
...  
Keyword(s):  
Small Molecule ◽  
Cathepsin D ◽  
Small Molecule Inhibitors ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Human Cathepsin
Sign in / Sign up

Export Citation Format

Share Document