scholarly journals Design, synthesis, andin vitrobiological evaluation of novel benzimidazole tethered allylidenehydrazinylmethylthiazole derivatives as potent inhibitors ofMycobacterium tuberculosis

MedChemComm ◽  
2019 ◽  
Vol 10 (1) ◽  
pp. 49-60 ◽  
Author(s):  
Goverdhan Surineni ◽  
Yamin Gao ◽  
Muzammal Hussain ◽  
Zhiyong Liu ◽  
Zhili Lu ◽  
...  
Keyword(s):  
Lead Optimization ◽  
Chemical Probe ◽  
Design Synthesis ◽  
Ofmycobacterium Tuberculosis

Development of novel chemical probe for antitubercular lead optimization.

Design, synthesis and evaluation of peptide inhibitors ofMycobacterium tuberculosis ribonucleotide reductase

2007 ◽  
Vol 13 (12) ◽  
pp. 822-832 ◽  
Author(s):  
Johanna Nurbo ◽  
Annette K. Roos ◽  
Daniel Muthas ◽  
Erik Wahlström ◽  
Daniel J. Ericsson ◽  
...  
Keyword(s):  
Ribonucleotide Reductase ◽  
Peptide Inhibitors ◽  
Design Synthesis ◽  
Ofmycobacterium Tuberculosis

scholarly journals Chemoproteomic study uncovers HemK2/KMT9 as a new target for NTMT1 bisubstrate inhibitors

2021 ◽  
Author(s):  
Dongxing Chen ◽  
Ying Meng ◽  
Dan Yu ◽  
Nicholas Noinaj ◽  
Xiaodong Cheng ◽  
...  
Keyword(s):  
Rational Design ◽  
Biochemical Characterization ◽  
Potent Inhibitor ◽  
Protein Networks ◽  
Selective Inhibitors ◽  
Chemical Probe ◽  
Design Synthesis ◽  
Bisubstrate Inhibitors ◽  
Methyltransferase 1

Understanding the selectivity of methyltransferase inhibitors is important to dissect the functions of each methyltransferase target. From this perspective, here we report a chemoproteomic study to profile the selectivity of a potent protein N-terminal methyltransferase 1 (NTMT1) bisubstrate inhibitor NAH-C3-GPKK (Ki, app = 7 nM) in endogenous proteomes. First, we describe the rational design, synthesis, and biochemical characterization of a new chemical probe 6, a biotinylated analogue of NAH-C3-GPKK. Next, we systematically analyze protein networks that may selectively interact with the biotinylated probe 6 in concert with the competitor NAH-C3-GPKK. Besides NTMT1, the designated NTMT1 bisubstrate inhibitor NAH-C3-GPKK was found to also potently inhibit a methyltransferase complex HemK2-Trm112 (also known as KMT9-Trm112), highlighting the importance of systematic selectivity profiling. Furthermore, this is the first potent inhibitor for HemK2/KMT9 reported to date. Thus, our studies lay the foundation for future efforts towards the development of selective inhibitors for NTMT1 and HemK2/KMT9.

scholarly journals Hit-to-Lead Optimization of Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists with a Diphenylmethane-Scaffold: Design, Synthesis, and Biological Study

2016 ◽  
Vol 59 (21) ◽  
pp. 9825-9836 ◽  
Author(s):  
Grazia Chiellini ◽  
Giulia Nesi ◽  
Simona Sestito ◽  
Sara Chiarugi ◽  
Massimiliano Runfola ◽  
...  
Keyword(s):  
Lead Optimization ◽  
Biological Study ◽  
Scaffold Design ◽  
Design Synthesis ◽  
Trace Amine
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