Discovery of bioactive molecules from CuAAC click-chemistry-based combinatorial libraries

X Wang, B Huang, X Liu, P Zhan - Drug Discovery Today, 2016 - Elsevier
Highlights•Advances in the combination of the CuAAC reaction with direct screening.•Before
library assembly, the bioisosteric potential of 1, 2, 3-triazole should be confirmed.•The …

Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy

SM Myers, I Collins - Future medicinal chemistry, 2016 - Taylor & Francis
The kinesin class of microtubule-associated motor proteins present attractive anticancer
targets owing to their roles in key functions in dividing cells. Two interpolar mitotic kinesins …

Targeting centrosome amplification, an Achilles' heel of cancer

D Sabat-Pośpiech… - Biochemical Society …, 2019 - portlandpress.com
Due to cell-cycle dysregulation, many cancer cells contain more than the normal compliment
of centrosomes, a state referred to as centrosome amplification (CA). CA can drive …

Chemoenzymatic Synthesis of Optically Pure l- and d-Biarylalanines through Biocatalytic Asymmetric Amination and Palladium-Catalyzed Arylation

ST Ahmed, F Parmeggiani, NJ Weise, SL Flitsch… - ACS …, 2015 - ACS Publications
A chemoenzymatic approach was developed and optimized for the synthesis of a range of N-
protected nonnatural l-and d-biarylalanine derivatives. Starting from 4-bromocinnamic acid …

Targeting TACC3 represents a novel vulnerability in highly aggressive breast cancers with centrosome amplification

O Saatci, O Akbulut, M Cetin, V Sikirzhytski… - Cell Death & …, 2023 - nature.com
Centrosome amplification (CA) is a hallmark of cancer that is strongly associated with highly
aggressive disease and worse clinical outcome. Clustering extra centrosomes is a major …

Structural basis of human kinesin-8 function and inhibition

J Locke, AP Joseph, A Peña… - Proceedings of the …, 2017 - National Acad Sciences
Kinesin motors play diverse roles in mitosis and are targets for antimitotic drugs. The clinical
significance of these motors emphasizes the importance of understanding the molecular …

MicroCycle: An Integrated and Automated Platform to Accelerate Drug Discovery

CE Brocklehurst, E Altmann, C Bon… - Journal of medicinal …, 2024 - ACS Publications
We herein describe the development and application of a modular technology platform
which incorporates recent advances in plate-based microscale chemistry, automated …

[HTML][HTML] KIFC1: a promising chemotherapy target for cancer treatment?

YX Xiao, WX Yang - Oncotarget, 2016 - ncbi.nlm.nih.gov
The kinesin motor KIFC1 has been suggested as a potential chemotherapy target due to its
critical role in clustering of the multiple centrosomes found in cancer cells. In this regard …

Discovery of novel anti-HIV agents via Cu (I)-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry-based approach

P Gao, L Sun, J Zhou, X Li, P Zhan… - Expert Opinion on Drug …, 2016 - Taylor & Francis
Introduction: In recent years, a variety of new synthetic methodologies and concepts have
been proposed in the search for new pharmaceutical lead structures and optimization …

[HTML][HTML] The overexpression of KIFC1 was associated with the proliferation and prognosis of non-small cell lung cancer

Y Liu, P Zhan, Z Zhou, Z Xing, S Zhu, C Ma… - Journal of thoracic …, 2016 - ncbi.nlm.nih.gov
Background The kinesin family member C1 (KIFC1, also known as HSET) is a kinesin
superfamily protein (KIFs). Although KIFC1 acts as a crucial role in the development of …