Small Cause, Great Impact: Modification of the Guanidine Group in the RGD Motif Controls Integrin Subtype Selectivity

2015 ◽  
Vol 55 (4) ◽  
pp. 1540-1543 ◽  
Author(s):  
Tobias G. Kapp ◽  
Maximilian Fottner ◽  
Oleg V. Maltsev ◽  
Horst Kessler
Keyword(s):  
Guanidine Group ◽  
Rgd Motif ◽  
Subtype Selectivity ◽  
Impact Modification

scholarly journals Publisher Correction: Predicting Subtype Selectivity for Adenosine Receptor Ligands with Three-Dimensional Biologically Relevant Spectrum (BRS-3D)

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Song-Bing He ◽  
Ben Hu ◽  
Zheng-Kun Kuang ◽  
Dong Wang ◽  
De-Xin Kong
Keyword(s):  
Adenosine Receptor ◽  
Three Dimensional ◽  
Receptor Ligands ◽  
Biologically Relevant ◽  
Subtype Selectivity ◽  
Adenosine Receptor Ligands

An amendment to this paper has been published and can be accessed via a link at the top of the paper.

Formal total synthesis of (±)-7-deoxycylindrospermopsin and its 8-epi isomer

2021 ◽  
Author(s):  
Si-Qing Wang ◽  
Wei-Yi Qi ◽  
Xue-Song Yin ◽  
Bing-Feng Shi
Keyword(s):  
Total Synthesis ◽  
Guanidine Group ◽  
Marine Alkaloid

7-Deoxycylindrospermopsin is a member of cylindrospermopsin marine alkaloid containing a cyclic guanidine group. Herein, we present a concise formal total synthesis of (±)-7-deoxycylindrospermopsin in 14 steps from commercailly available 4-methoxypyridine....

scholarly journals Pharmacologic profiling of patient-derived xenograft models of primary treatment-naïve triple-negative breast cancer

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Reid T. Powell ◽  
Abena Redwood ◽  
Xuan Liu ◽  
Lei Guo ◽  
Shirong Cai ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Triple Negative Breast Cancer ◽  
Triple Negative ◽  
Human Tumor ◽  
The United States ◽  
Glutathione Metabolism ◽  
Subtype Selectivity ◽  
Patient Derived Xenograft ◽  
Treatment Naïve ◽  
Xenograft Models

Abstract Triple-negative breast cancer (TNBC) accounts for 15–20% of breast cancer cases in the United States, lacks targeted therapeutic options, and is associated with a 40–80% risk of recurrence. Thus, identifying actionable targets in treatment-naïve and chemoresistant TNBC is a critical unmet medical need. To address this need, we performed high-throughput drug viability screens on human tumor cells isolated from 16 patient-derived xenograft models of treatment-naïve primary TNBC. The models span a range of TNBC subtypes and exhibit a diverse set of putative driver mutations, thus providing a unique patient-derived, molecularly annotated pharmacologic resource that is reflective of TNBC. We identified therapeutically actionable targets including kinesin spindle protein (KSP). The KSP inhibitor targets the mitotic spindle through mechanisms independent of microtubule stability and showed efficacy in models that were resistant to microtubule inhibitors used as part of the current standard of care for TNBC. We also observed subtype selectivity of Prima-1Met, which showed higher levels of efficacy in the mesenchymal subtype. Coupling pharmacologic data with genomic and transcriptomic information, we showed that Prima-1Met activity was independent of its canonical target, mutant p53, and was better associated with glutathione metabolism, providing an alternate molecularly defined biomarker for this drug.

scholarly journals Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity

Cell ◽  
2017 ◽  
Vol 168 (5) ◽  
pp. 867-877.e13 ◽  
Author(s):  
Alisa Glukhova ◽  
David M. Thal ◽  
Anh T. Nguyen ◽  
Elizabeth A. Vecchio ◽  
Manuela Jörg ◽  
...  
Keyword(s):  
Adenosine A1 Receptor ◽  
Subtype Selectivity ◽  
Adenosine A1 ◽  
A1 Receptor

Dualsteric Muscarinic Antagonists–Orthosteric Binding Pose Controls Allosteric Subtype Selectivity

2014 ◽  
Vol 57 (15) ◽  
pp. 6739-6750 ◽  
Author(s):  
Jens Schmitz ◽  
Dorina van der Mey ◽  
Marcel Bermudez ◽  
Jessica Klöckner ◽  
Ramona Schrage ◽  
...  
Keyword(s):  
Muscarinic Antagonists ◽  
Subtype Selectivity
Sign in / Sign up

Export Citation Format

Share Document