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septembre 2022 – Page 32 – ChemDigest

Mois : septembre 2022

Discovery and Structural and Functional Characterization of a Novel A‑Superfamily Conotoxin Targeting α9α10 Nicotinic Acetylcholine Receptor

Par / 1 septembre 2022 / chemical_biology

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ACS Chemical Biology

ACS Chemical Biology: Latest Articles (ACS Publications)
Authors: Qiuyuan Huang, Xin Chu, Haoran Zhang, Shuo Yu, Longxiao Zhang, Xuerong Zhang, Rilei Yu, Chenyun Guo, and Qiuyun Dai
dx.doi.org/https://doi.org/10.1021/acschembio.2c00315

Advancing Scalable Chemistry toward Novel CELMoDs: Process Development for the Synthesis of CC-90009

Par / 1 septembre 2022 / Non classé

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Organic Process Research & Development
Organic Process Research & Development: Latest Articles (ACS Publications)

Authors: Michael J. Zacuto, Michael J. Williams, Weihong Zhang, Jianxin Han, Marie G. Beauchamps, Mohit Kothare, William Konnecke, Randi Smith, and Gregg Feigelson
dx.doi.org/https://doi.org/10.1021/acs.oprd.2c00199

Real-Time Cellular Thermal Shift Assay to Monitor Target Engagement

Par / 1 septembre 2022 / chemical_biology

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ACS Chemical Biology

ACS Chemical Biology: Latest Articles (ACS Publications)
Authors: Tino W. Sanchez, Michael H. Ronzetti, Ashley E. Owens, Maria Antony, Ty Voss, Eric Wallgren, Daniel Talley, Krishna Balakrishnan, Sebastian E. Leyes Porello, Ganesha Rai, Juan J. Marugan, Samuel G. Michael, Bolormaa Baljinnyam, Noel Southall, Anton Simeonov, and Mark J. Henderson
dx.doi.org/https://doi.org/10.1021/acschembio.2c00334

Scalable Process of Spiro(cyclopropane)oxazepane Pyridine Carboxylic Acid through Kulinkovich, Mitsunobu, and Pd-Catalyzed Intramolecular C–N Coupling

Par / 1 septembre 2022 / Non classé

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Organic Process Research & Development
Organic Process Research & Development: Latest Articles (ACS Publications)

Authors: Bo Qu, Jaehee Lee, Lifen Wu, Anjan K. Saha, Guisheng Li, Yibo Xu, Zhulin Tan, Jason Brazzillo, Nizar Haddad, Scott Pennino, Sonia Rodriguez, Jon C. Lorenz, Rogelio Frutos, Kanwar P. S. Sidhu, Xiao-Jun Wang, Yongda Zhang, Chris H. Senanayake, and Jinhua J. Song
dx.doi.org/https://doi.org/10.1021/acs.oprd.2c00221

Highly Potent and Oral Macrocyclic Peptides as a HIV‑1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization

Par / 1 septembre 2022 / medchem

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Yoshifumi Kusumoto, Kyohei Hayashi, Soichiro Sato, Toru Yamada, Iori Kozono, Zenzaburo Nakata, Naoya Asada, Shungo Mitsuki, Ayahisa Watanabe, Chiaki Wakasa-Morimoto, Kentaro Uemura, Shuhei Arita, Shinobu Miki, Tohru Mizutare, and Hidenori Mikamiyama
dx.doi.org/http://dx.doi.org/10.1021/acsmedchemlett.2c00310

Phase Separation of Heterogeneous Nuclear Ribonucleoprotein A1 upon Specific RNA‐Binding Observed by Magnetic Resonance

Par / 1 septembre 2022 / Non classé
Phase Separation of Heterogeneous Nuclear Ribonucleoprotein A1 upon Specific RNA-Binding Observed by Magnetic Resonance**

An ensemble model of free dispersed full-length heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1) was generated from magnetic resonance data based on site-directed spin labelling and from a small-angle x-ray scattering curve. Electron paramagnetic resonance spectroscopy combined with this model provides insight into the interplay of specific single-stranded RNA recognition by hnRNP A1 and its liquid-liquid phase separation.

Abstract

Interaction of heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1) with specific single-stranded RNA and its relation to liquid-liquid phase separation (LLPS) were studied in vitro by magnetic resonance based on site-directed spin labelling. An ensemble model of dispersed hnRNP A1 in the absence of RNA was derived from distance distributions between spin labelled sites and small angle X-ray scattering. This model revealed a compact state of the low-complexity domain and its interaction with the RNA recognition motifs. Paramagnetic relaxation enhancement NMR spectroscopy confirmed this interaction. Addition of RNA to dispersed hnRNP A1 induced liquid-droplet formation. Such LLPS depended on RNA concentration and sequence, with continuous wave EPR spectroscopy showing an influence of RNA point mutations on local protein dynamics. We propose that an interplay of sequence-specific RNA binding and LLPS contributes to regulation of specific RNA segregation during stress response.

Wiley: Angewandte Chemie International Edition: Table of Contents
Authors: Irina Ritsch, Elisabeth Lehmann, Leonidas Emmanouilidis, Maxim Yulikov, Frédéric Allain, Gunnar Jeschke
onlinelibrary.wiley.com/doi/10.1002/anie.202204311

Facile Access to Far‐Red Fluorescent Probes with Through‐Space Charge‐Transfer Effects for In Vivo Two‐Photon Microscopy of the Mouse Cerebrovascular System

Par / 1 septembre 2022 / Non classé
Facile Access to Far-Red Fluorescent Probes with Through-Space Charge-Transfer Effects for In Vivo Two-Photon Microscopy of the Mouse Cerebrovascular System

Complexes formed between aggregation-induced emission (AIE) acceptors and arylamine donors showed through-space charge transfer as well as a “twist+twist” interaction between the acceptor and the donor. Owing to these properties, the complexes served as far-red fluorescent nanoprobes with two-photon excitation. The probe was applied to in vivo imaging of the mouse cerebrovascular system.

Abstract

Much effort has been devoted to the generation of fluorescent probes by synthetic approaches. In this study, we developed a facile strategy to construct far-red fluorescent probes based on through-space charge transfer within complexes of acceptors and donors and their “twist+twist” interactions. Owing to their rare two-photon excitation property, the complexes could be used for in vivo imaging of the mouse cerebrovascular system.

Wiley: Angewandte Chemie International Edition: Table of Contents
Authors: Yingjuan Hong, Weihang Geng, Tian Zhang, Guangshuai Gong, Chongyang Li, Canze Zheng, Feng Liu, Jun Qian, Ming Chen, Ben Zhong Tang
onlinelibrary.wiley.com/doi/10.1002/anie.202209590