Results 121 to 130 of about 6,512,999 (388)

Fast Screening of Inhibitor Binding/Unbinding Using Novel Software Tool CaverDock

Frontiers in Chemistry, 2019
Protein tunnels and channels are attractive targets for drug design. Drug molecules that block the access of substrates or release of products can be efficient modulators of biological activity. Here, we demonstrate the applicability of a newly developed
Gaspar P. Pinto, Gaspar P. Pinto, Ondrej Vavra, Ondrej Vavra, Jiri Filipovic, Jan Stourac, Jan Stourac, David Bednar, David Bednar, Jiri Damborsky, Jiri Damborsky   +10 more
doaj   +1 more source

Mechanisms of resistance to immune checkpoint inhibitors

British Journal of Cancer, 2018
Immune checkpoint inhibitors (ICI) targeting CTLA-4 and the PD-1/PD-L1 axis have shown unprecedented clinical activity in several types of cancer and are rapidly transforming the practice of medical oncology.
R. Jenkins, D. Barbie, K. Flaherty
semanticscholar   +1 more source

Aurora kinase A drives the evolution of resistance to third-generation EGFR inhibitors in lung cancer. [PDF]

, 2019
Although targeted therapies often elicit profound initial patient responses, these effects are transient due to residual disease leading to acquired resistance.
A Hübner, AB D’Assoro, AJ Lee, AN Hata, Andrei Goga, Andrew D. Simmons, Angel Ku, AS Nikonova, Ashley Maynard, B Melichar, CA Eberlein, CK Lee, CM Blakely, CM Blakely, Collin M. Blakely, D Ercan, DB Costa, F Varghese, Frank McCormick, Golzar Hemmati, Gregor Krings, Hayley J. Donnella, Henry J. Haringsma, J Chen, J Fu, Jacqueline Galeas, JJ Chabon, Jonathan Kuhn, Julia Rohrberg, Julia Rotow, K Shien, Khyati N. Shah, KS Thress, L Li, Liliane Robillard, LV Sequist, LV Sequist, M Moustafa-Kamal, M Ramirez, Maria M. Martins, MJ Niederst, MS Cragg, MW Karaman, OJ Gruss, PA Jänne, R Rosell, RA Burrell, Roma Bhatt, S Anand, S Stewart, Sophie Dumont, Sourav Bandyopadhyay, SV Sharma, Swati Kaushik, T Sharifnia, TC Chou, TG Bivona, TG Bivona, Thomas C. Harding, TM Kim, Trever G. Bivona, V Bavetsias, Victor Olivas, Victoria E. Wang, Y Zhou, Z Piotrowska, Z Yang   +66 more
core   +1 more source

P‐glycoprotein modulates the fluidity gradient of the plasma membrane of multidrug resistant CHO cells

FEBS Letters, EarlyView.
To explore the impact of the overexpression of the multidrug‐transporter P‐glycoprotein (ABCB1) on membrane fluidity, we compared the transversal gradient of mobility and microviscosity in plasma membranes of drug‐sensitive Chinese hamster ovary cells (AuxB1) and their multidrug‐resistant derivatives (B30) using the fluorescent n‐(9‐anthroyloxy) fatty ...
Roger Busche, John R. Riordan, Burkhard Tümmler   +2 more
wiley   +1 more source

Evolutionary interplay between viruses and R‐loops

FEBS Letters, EarlyView.
Viruses interact with specialized nucleic acid structures called R‐loops to influence host transcription, epigenetic states, latency, and immune evasion. This Perspective examines the roles of R‐loops in viral replication, integration, and silencing, and how viruses co‐opt or avoid these structures.
Zsolt Karányi, Zita Képes, Zoltán Szabó, Eszter Csoma, Lóránt Székvölgyi   +4 more
wiley   +1 more source

Evolution of PIKK family kinase inhibitors: A new age cancer therapeutics

Frontiers in Bioscience-Landmark, 2020
Phosphatidylinositol-3 kinase-related kinases (PIKKs) belong to a family of atypical serine/threonine kinases in humans. They actively participate in a diverse set of cellular functions such as meiotic, V(D)J recombination, chromosome maintenance, DNA ...
Althaf Shaik, Sivapriya Kirubakaran
doaj   +1 more source

A high-throughput mass spectrometric assay for discovery of human lipoxygenase inhibitors and allosteric effectors. [PDF]

, 2015
Lipoxygenases (LOXs) regulate inflammation through the production of a variety of molecules whose specific downstream effects are not entirely understood due to the complexity of the inflammation pathway.
Holman, Theodore R, Jameson, J Brian, Kenyon, Victor   +2 more
core   +1 more source

Disruption of SETD3‐mediated histidine‐73 methylation by the BWCFF‐associated β‐actin G74S mutation

FEBS Letters, EarlyView.
The β‐actin G74S mutation causes altered interaction of actin with SETD3, reducing histidine‐73 methylation efficiency and forming two distinct actin variants. The variable ratio of these variants across cell types and developmental stages contributes to tissue‐specific phenotypical changes. This imbalance may impair actin dynamics and mechanosensitive
Anja Marquardt, Marcus S. Münchhoff, Jacqueline Krohn, Philip M. Palarz, Manuel H. Taft, Johannes N. Greve, Nataliya Di Donato, Falk F. R. Buettner, Dietmar J. Manstein   +8 more
wiley   +1 more source

Healthy nutrition barriers: perception of adults male

Payesh, 2012
Objective (s): Existing data show a considerable prevalence of non communicable diseases risk factors and their rising trend in our country. Unhealthy nutrition is an important underlying factor for mentioned diseases.
Fahimeh Ramezani Tehrani, Maryam Farahmand, Parisa Amiri, Arash Ghanbarian, Fereidoun Azizi   +4 more
doaj  

Insights into pegRNA design from editing of the cardiomyopathy‐associated phospholamban R14del mutation

FEBS Letters, EarlyView.
This study reveals how prime editing guide RNA (pegRNA) secondary structure and reverse transcriptase template length affect prime editing efficiency in correcting the phospholamban R14del cardiomyopathy‐associated mutation. Insights support the design of structurally optimized enhanced pegRNAs for precise gene therapy.
Bing Yao, Qiangbing Yang, Christian J.B. Snijders Blok, Mark A. Daniels, Pieter A. Doevendans, Raymond Schiffelers, Joost P.G. Sluijter, Zhiyong Lei   +7 more
wiley   +1 more source