Results 41 to 50 of about 50,722 (204)

Cryo-EM structures of the tubulin cofactors reveal the molecular basis of alpha/beta-tubulin biogenesis

Nature Communications
Microtubule polarity and dynamic polymerization arise from the self-association properties of the αβ-tubulin heterodimer. For decades, it has remained unclear how the tubulin cofactors TBCD, TBCE, TBCC, and the Arl2 GTPase mediate the biogenesis of αβ ...
Aryan Taheri, Zhoaqian Wang, Bharti Singal, Fei Guo, Jawdat Al-Bassam   +4 more
doaj   +1 more source

Novel Suicide Ligands of Tubulin Arrest Cancer Cells in S-Phase

Neoplasia: An International Journal for Oncology Research, 1999
It is presently accepted that the mechanism of action for all anti-tumor tubulin ligands involves the perturbation of microtubule dynamics during the G2/M phase of cell division and subsequent entry into apoptosis 1].
Ashley Davis, Jian-Dong Jiang, Kim M. Middleton, Yue Wang, Imre Weisz, Yi-He Ling, J. George Bekesi   +6 more
doaj   +1 more source

Methoxy and bromo scans on N-(5-methoxyphenyl) methoxybenzenesulphonamides reveal potent cytotoxic compounds, especially against the human breast adenocarcinoma MCF7 cell line

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Thirty seven N-(5-methoxyphenyl)-4-methoxybenzenesulphonamide with methoxy or/and bromo substitutions (series 1-4) and with different substituents on the sulphonamide nitrogen have been synthesised.
Myriam González, María Ovejero-Sánchez, Alba Vicente-Blázquez, Manuel Medarde, Rogelio González-Sarmiento, Rafael Peláez   +5 more
doaj   +1 more source

Peripheral lysosomes recruit PLEKHG3 to focal adhesions and restrain protrusion dynamics

FEBS Letters, EarlyView.
Proximity‐dependent labeling at the LAMTOR complex revealed the Rho GEF PLEKHG3 as a lysosome‐proximal protein directing the study toward the influence of lysosome positioning on actin dynamics and cell motility. We show that PLEKHG3 colocalizes with lysosomes at focal adhesion sites and observe that forced peripheral dispersion of lysosomes hinders ...
Rainer Ettelt, Ana‐Maria Sandru, Georg Vucak, Sebastian Didusch, Biljana Riemelmoser, Karin Ehrenreiter, Markus Hartl, Lukas A. Huber, Manuela Baccarini   +8 more
wiley   +1 more source

Design, synthesis, in silico studies, and apoptotic antiproliferative activity of novel thiazole-2-acetamide derivatives as tubulin polymerization inhibitors

Frontiers in Chemistry
IntroductionTubulin polymerization inhibitors have emerged as interesting anticancer therapies. We present the design, synthesis, and structural elucidation of novel thiazole-based derivatives to identify novel tubulin inhibitors with potent ...
Lamya H. Al-Wahaibi, Ali M. Elshamsy, Taha F. S. Ali, Bahaa G. M. Youssif, Stefan Bräse, Mohamed Abdel-Aziz, Nawal A. El-Koussi, Nawal A. El-Koussi   +7 more
doaj   +1 more source

Exploitation of the protein tubulin for controlling African trypanosomiasis [PDF]

, 2005
This thesis presents the results of an investigation into the structural protein, tubulin, as a potential target for anti-trypanosomatid drug discovery and vaccine development.
Giles, Natalie
core  

Loss of IGF‐1R impairs DNA‐PKcs recruitment to chromatin leading to defective end‐joining

Molecular Oncology, EarlyView.
IGF‐1R promotes radioresistance by facilitating DNA‐PKcs recruitment to chromatin, enabling non‐homologous end‐joining (NHEJ) repair of double‐strand breaks. Inhibition or loss of IGF‐1R disrupts this recruitment to damage sites, driving compensatory reliance on microhomology‐mediated end‐joining (MMEJ) repair.
Matthew O. Ellis, Jack V. Mills, Wojciech Niedzwiedz, Valentine M. Macaulay   +3 more
wiley   +1 more source

Design, synthesis and evaluation of dihydro-1H-indene derivatives as novel tubulin polymerisation inhibitors with anti-angiogenic and antitumor potency

Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Angiogenesis plays an important role in tumour generation and progression, which is used to supply nutrients and metastasis. Herein, a series of novel dihydro-1H-indene derivatives were designed and evaluated as tubulin polymerisation inhibitors by ...
Shengtao Xu, Yijun Sun, Peng Wang, Yuchen Tan, Lei Shi, Jian Chen   +5 more
doaj   +1 more source

Mechanism of Tubulin Oligomers and Single-Rings Disassembly Catastrophe [PDF]

, 2022
Cold tubulin dimers coexist with tubulin oligomers and single-rings. These structures are involved in microtubule assembly, however, their dynamics are poorly understood.
Raviv, Dharan, Israel, Ringel, Uri, Raviv, Yael, Levi-Kalisman, Asaf, Shemesh, Avi, Ginsburg   +5 more
core   +2 more sources

Finding novel vulnerabilities of hypomorphic BRCA1 alleles

Molecular Oncology, EarlyView.
Synthetic lethality screens performed to identify novel vulnerabilities often model complete gene loss, thereby overlooking patient‐derived hypomorphic mutations. In this study, we have performed genome‐wide CRISPR screens on BRCA1 hypomorphic mutations, showing BRCA1I26A behaves like wild‐type, while BRCA1R1699Q mimics deficiency. Furthermore, we have
Anne Schreuder, Klaas de Lint, Hồ Mỹ Phúc Võ, Mariana M. Góis, Rosalie A. Kampen, Marta San Martin Alonso, Ilse Nootenboom, Veronica Garzero, Tiemen J. Wendel, Rob M. F. Wolthuis, Sylvie M. Noordermeer   +10 more
wiley   +1 more source