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40 Newest Publications about the topic target validation


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1,3,5-triazaspiro[5.5]undeca-2,4-dienes as selective Mycobacterium tuberculosis dihydrofolate reductase inhibitors with potent whole cell activity

24-Dec-2017 | Author(s): Xuan Yang, Wassihun Wedajo, Yoshiyuki Yamada, Sue-Li Dahlroth, Jason Jun-Long Neo, Thomas Dic ..., European Journal of Medicinal Chemistry, 2017

Publication date: 20 January 2018 Source:European Journal of Medicinal Chemistry, Volume 144 Author(s): Xuan Yang, Wassihun Wedajo, Yoshiyuki Yamada, Sue-Li Dahlroth, Jason Jun-Long Neo, Thomas Dick, Wai-Keung Chui The emergence of multi- and extensively-drug resistant ...


Therapeutic investigations of novel indoxyl-based indolines: A drug target validation and Structure-Activity Relationship of angiotensin-converting enzyme inhibitors with cardiovascular regulation and thrombolytic potential

14-Oct-2017 | Author(s): A. Manikandan, Pearl Moharil, M. Sathishkumar, C. Muñoz-Garay, A. Sivakumar, European Journal of Medicinal Chemistry, 2017

Publication date: 1 December 2017 Source:European Journal of Medicinal Chemistry, Volume 141 Author(s): A. Manikandan, Pearl Moharil, M. Sathishkumar, C. Muñoz-Garay, A. Sivakumar A family of 12 members of Naphthalene-2-ol-indolin-2-one-thiocarbamides (5a-l) with pharmacological ...


An av‐RGD integrin inhibitor toolbox: drug discovery insight, challenges and opportunities

25-Sep-2017 | Richard Hatley, Simon Macdonald, Robert Slack, Joelle Le, Steve Ludbrook, Pauline Lukey, Angewandte Chemie International Edition, 2017

There is a requirement for efficacious and safe medicines to treat diseases with high unmet need. The resurgence in av RGD integrin inhibitor drug discovery is poised to contribute to this requirement. However, drug discovery in the av integrin space is notoriously difficult due to the ...


Ruthenium Promoted On-DNA Ring-Closing Metathesis and Cross-Metathesis

09-Jun-2017 | Xiaojie Lu; Lijun Fan; Christopher B. Phelps; Christopher P. Davie; Christine P. Donahue, Bioconjugate Chemistry, 2017

DNA-encoded library technology (ELT) is now widely used in pharmaceutical, biotechnological, and academic research for hit identification and target validation. New on-DNA reactions are keys to exploring greater chemical space and accessing challenging chemotypes such as configurationally ...


Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain

12-May-2017 | R. Aldrin Denny; Andrew C. Flick; Jotham Coe; Jonathan Langille; Arindrajit Basak; Shenping Liu; Ingrid Stock; Parag ..., Journal of Medicinal Chemistry, 2017

Chemical probes are required for preclinical target validation to interrogate novel biological targets and pathways. Selective inhibitors of the CREB binding protein (CREBBP)/EP300 bromodomains are required to facilitate the elucidation of biology associated with these important epigenetic ...


M1 aminopeptidases as drug targets: broad applications or therapeutic niche?

11-Jan-2017 | Nyssa Drinkwater, Jisook Lee, Wei Yang, Tess R. Malcolm, Sheena McGowan, FEBS Journal, 2017

Abstract M1 aminopeptidase enzymes are a diverse family of metalloenzymes characterized by conserved structure and reaction specificity. Excluding viruses, M1 aminopeptidases are distributed throughout all phyla, and have been implicated in a wide range of functions including cell maintenance, ...


Selectivity Determination of a Small Molecule Chemical Probe Using Protein Microarray and Affinity Capture Techniques

17-Aug-2016 | Erik C. Hett; Robert E. Kyne, Jr.; Ariamala Gopalsamy; Michael A. Tones; Hua Xu; Guene L. Thio; Edward Nolan; Lyn H. ..., Journal of Combinatorial Chemistry, 2016

Small molecule selectivity is an essential component of candidate drug selection and target validation. New technologies are required to better understand off-target effects, with particular emphasis needed on broad protein profiling. Here, we describe the use of a tritiated chemical probe and a ...


Therapeutic Potential of Foldamers: From Chemical Biology Tools To Drug Candidates?

29-Jul-2016 | Ranganath Gopalakrishnan; Andrey I. Frolov; Laurent Knerr; William J. Drury, III; Eric Valeur, Journal of Medicinal Chemistry, 2016

Over the past decade, foldamers have progressively emerged as useful architectures to mimic secondary structures of proteins. Peptidic foldamers, consisting of various amino acid based backbones, have been the most studied from a therapeutic perspective, while polyaromatic foldamers have barely ...


Clickable 4‐Oxo‐β‐lactam‐Based Selective Probing for Human Neutrophil Elastase Related Proteomes

28-Jul-2016 | Eduardo F. P. Ruivo, Lídia M. Gonçalves, Luís A. R. Carvalho, Rita C. Guedes, Stefan Hofbauer, José A. Brito, Margar ..., ChemMedChem, 2016

Abstract Human neutrophil elastase (HNE) is a serine protease associated with several inflammatory processes such as chronic obstructive pulmonary disease (COPD). The precise involvement of HNE in COPD and other inflammatory disease mechanisms has yet to be clarified. Herein we report a ...


Focusing on probe-modified peptides: a quick and effective way for target identification

19-Jul-2016 | Huan Sun; Yan Ren; Weijie Hou; Lin Li; Fanqi Zeng; Sisi Li; Yongfen Ma; Xiao Liu; She Chen; Zhiyuan Zhang, Chemical Communication, 2016

A new efficient method focusing on probe-modified peptides was developed to identify the target protein and modification site of a hit compound or a drug. This method exhibited high click conjugation efficiency and few false-positive results. The modification site further facilitated target ...


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