Pharmacology and Toxicology

Discovery and biological evaluation of a potent small molecule CRM1 inhibitor for its selective ablation of extranodal NK/T cell lymphoma

1. He Liu
2. Meisuo Liu
3. Xibao Tian
4. Haina Wang
5. Jiujiao Gao
6. Hanrui Li
7. Zhehuan Zhao
8. Yu Liu
9. Caigang Liu
10. Xuan Chen
11. Yongliang Yang

• Curated by eLife

  eLife assessment

  This study reports a valuable finding on the discovery and evaluation of a potent small molecule inhibitor for CRM1 that may be important to treat extranodal NK/T cell lympohma (ENKTL). The evidence supporting the claims of the authors is solid that reflects an important finding for novel CRM1 inhibitors to treat ENKTL, although additional experimental evidence is needed. The work will be of interest to cancer biologists working on ENKTL.

Reviewed by eLife

A novel triptolide analog downregulates NF-κB and induces mitochondrial apoptosis pathways in human pancreatic cancer

1. Qiaomu Tian
2. Peng Zhang
3. Yihan Wang
4. Youhui Si
5. Dengping Yin
6. Christopher R Weber
7. Melissa L Fishel
8. Karen E Pollok
9. Bo Qiu
10. Fei Xiao
11. Anita S Chong

• Curated by eLife

  eLife assessment

  This useful manuscript presents a new therapeutic formulation and these solid findings have potential clinical significance as the efficacy of CK21 is relevant in various pancreatic cancer models.Further validation studies would help to strengthen the findings.

Reviewed by eLife

Death by a thousand cuts through kinase inhibitor combinations that maximize selectivity and enable rational multitargeting

1. Ian R Outhwaite
2. Sukrit Singh
3. Benedict-Tilman Berger
4. Stefan Knapp
5. John D Chodera
6. Markus A Seeliger

• Curated by eLife

  eLife assessment

  This study presents a valuable finding on an alternative method that combines multiple inhibitors to maximize on-target inhibition and minimize off-target inhibition. The evidence supporting the claims of the authors is solid, although a proper validation of the methodology could strengthen the paper. The work will be of interest to scientists working in the field of drug discovery, particularly in the field of kinase inhibitors.

Reviewed by eLife

Optical Control of G-Actin with a Photoswitchable Latrunculin

1. Nynke A. Vepřek
2. Madeline H. Cooper
3. Laura Laprell
4. Emily Jie-Ning Yang
5. Sander Folkerts
6. Ruiyang Bao
7. Malgorzata Boczkowska
8. Nicholas J. Palmer
9. Roberto Dominguez
10. Thomas G. Oertner
11. Liza A. Pon
12. J. Bradley Zuchero
13. Dirk H. Trauner

Reviewed by preLights

The G protein biased serotonin 5-HT 2A receptor agonist lisuride exerts anti-depressant drug-like activities in mice

1. Vladimir M. Pogorelov
2. Ramona M. Rodriguiz
3. Bryan L. Roth
4. William C. Wetsel

Reviewed by Arcadia Science

The herbicide acetochlor causes lipid peroxidation by inhibition of glutathione peroxidase 4

1. Fahmi Mesmar
2. Maram Muhsen
3. Jason P. Tourigny
4. Jason M. Tennessen
5. Maria Bondesson

Reviewed by PREreview

Natural and engineered mediators of desiccation tolerance stabilize Human Blood Clotting Factor VIII in a dry state

1. Maxwell H. Packebush
2. Silvia Sanchez-Martinez
3. Sourav Biswas
4. KC Shraddha
5. Kenny Nguyen
6. Thomas C. Boothby

Reviewed by Arcadia Science

A generic binding pocket for small molecule IKs activators at the extracellular inter-subunit interface of KCNQ1 and KCNE1 channel complexes

1. Magnus Chan
2. Harutyun Sahakyan
3. Jodene Eldstrom
4. Daniel Sastre
5. Yundi Wang
6. Ying Dou
7. Marc Pourrier
8. Vitya Vardanyan
9. David Fedida

• Curated by eLife

  eLife assessment

  By combining electrophysiological analysis of mutant channels and molecular dynamics simulations, this important study identifies a common binding site for two structurally distinct activators of KCNQ1-KCNE1 channels. The findings represent an important advance for the field, with convincing functional and computational data to support the claims. The work will be of interest to those studying the binding of small molecule drugs to membrane protein complexes.

Reviewed by eLife

Identifying SARS-CoV-2 Entry Inhibitors through Drug Repurposing Screens of SARS-S and MERS-S Pseudotyped Particles

1. Catherine Z. Chen
2. Miao Xu
3. Manisha Pradhan
4. Kirill Gorshkov
5. Jennifer D. Petersen
6. Marco R. Straus
7. Wei Zhu
8. Paul Shinn
9. Hui Guo
10. Min Shen
11. Carleen Klumpp-Thomas
12. Samuel G. Michael
13. Joshua Zimmerberg
14. Wei Zheng
15. Gary R. Whittaker

Reviewed by ScreenIT

A Strategy to Treat COVID‐19 Disease With Targeted Delivery of Inhalable Liposomal Hydroxychloroquine: A Preclinical Pharmacokinetic Study

1. Tien‐Tzu Tai
2. Tzung‐Ju Wu
3. Huey‐Dong Wu
4. Yi‐Chen Tsai
5. Hui‐Ting Wang
6. An‐Min Wang
7. Sheue‐Fang Shih
8. Yee‐Chun Chen

Reviewed by ScreenIT