Click chemistry for drug development and diverse chemical–biology applications

P Thirumurugan, D Matosiuk, K Jozwiak - Chemical reviews, 2013 - ACS Publications
Chemistry, traditionally being the science of synthesis and structural manipulations of
molecules, has gradually undertaken the more challenging task of biology-oriented …

Diazirine based photoaffinity labeling

L Dubinsky, BP Krom, MM Meijler - Bioorganic & medicinal chemistry, 2012 - Elsevier
Diazirines are among the smallest photoreactive groups that form a reactive carbene upon
light irradiation. This feature has been widely utilized in photoaffinity labeling to study ligand …

Direct and cost-efficient hyperpolarization of long-lived nuclear spin states on universal 15N2-diazirine molecular tags

T Theis, GX Ortiz Jr, AWJ Logan, KE Claytor, Y Feng… - Science …, 2016 - science.org
Conventional magnetic resonance (MR) faces serious sensitivity limitations which can be
overcome by hyperpolarization methods, but the most common method (dynamic nuclear …

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

DS Johnson, E Weerapana… - Future medicinal …, 2010 - Taylor & Francis
This article presents several covalent inhibitors, including examples of successful drugs, as
well as highly selective, irreversible inhibitors of emerging therapeutic targets, such as fatty …

The life of pi star: exploring the exciting and forbidden worlds of the benzophenone photophore

G Dorman, H Nakamura, A Pulsipher… - Chemical …, 2016 - ACS Publications
The widespread applications of benzophenone (BP) photochemistry in biological chemistry,
bioorganic chemistry, and material science have been prominent in both academic and …

Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes

H Shi, CJ Zhang, GYJ Chen… - Journal of the American …, 2012 - ACS Publications
Protein kinases (PKs) play an important role in the development and progression of cancer
by regulating cell growth, survival, invasion, metastasis, and angiogenesis. Dasatinib (BMS …

Development and mechanism of γ-secretase modulators for Alzheimer's disease

CJ Crump, DS Johnson, YM Li - Biochemistry, 2013 - ACS Publications
γ-Secretase is an aspartyl intramembranal protease composed of presenilin, Nicastrin,
Aph1, and Pen2 with 19 transmembrane domains. γ-Secretase cleaves the amyloid …

γ‐Secretase inhibitors and modulators for Alzheimer's disease

MS Wolfe - Journal of neurochemistry, 2012 - Wiley Online Library
J. Neurochem.(2012) 120 (Suppl. 1), 89–98. Abstract γ‐Secretase is a membrane
embedded aspartyl protease complex with presenilin as the catalytic component. Along with …

Current advances of carbene-mediated photoaffinity labeling in medicinal chemistry

SS Ge, B Chen, YY Wu, QS Long, YL Zhao, PY Wang… - RSC …, 2018 - pubs.rsc.org
Photoaffinity labeling (PAL) in combination with a chemical probe to covalently bind its target
upon UV irradiation has demonstrated considerable promise in drug discovery for identifying …

Recent advances in target characterization and identification by photoaffinity probes

J Sumranjit, SJ Chung - Molecules, 2013 - mdpi.com
Target identification of biologically active molecules such as natural products, synthetic
small molecules, peptides, and oligonucleotides mainly relies on affinity chromatography …