Results 41 to 50 of about 1,650,445 (352)

Auto In Silico Ligand Directing Evolution to Facilitate the Rapid and Efficient Discovery of Drug Lead

iScience, 2020
Summary: Motivated by the growing demand for reducing the chemical optimization burden of H2L, we developed auto in silico ligand directing evolution (AILDE, http://chemyang.ccnu.edu.cn/ccb/server/AILDE), an efficient and general approach for the rapid ...
Fengxu Wu, Linsheng Zhuo, Fan Wang, Wei Huang, Gefei Hao, Guangfu Yang   +5 more
doaj   +1 more source

The anti‐CRISPR protein AcrIE8.1 inhibits the type I‐E CRISPR‐Cas system by directly binding to the Cascade subunit Cas11

FEBS Letters, EarlyView.
In this study, we present the structure of AcrIE8.1, a previously uncharacterized anti‐CRISPR protein that inhibits the type I‐E CRISPR‐Cas system. Through a combination of structural and biochemical analyses, we demonstrate that AcrIE8.1 directly binds to the Cas11 subunit of the Cascade complex to inhibit the CRISPR‐Cas system.
Young Woo Kang, Hyun Ho Park
wiley   +1 more source

Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity

Heliyon, 2019
Poly(amidoamine) and Poly(propylenimine) dendrimers with different generations and peripheral groups were studied as solubility enhancers and nanocarriers for 7-bromo-2-hydroxy-phenazine N5,N10-dioxide.
Nahir Dib, Luciana Fernández, Marisa Santo, Luis Otero, Fabrisio Alustiza, Ana Cecilia Liaudat, Pablo Bosch, M. Laura Lavaggi, Hugo Cerecetto, Mercedes González   +9 more
doaj   +1 more source

Key Green Chemistry research areas from a pharmaceutical manufacturers’ perspective revisited

, 2018
In 2007 the members of the ACS Green Chemistry Institute® Pharmaceutical Roundtable assembled a list of key green chemistry research areas to both identify transformations that would benefit from improvements in process greenness and to encourage ...
M. Bryan, P. Dunn, D. Entwistle, F. Gallou, S. Koenig, J. Hayler, M. Hickey, S. Hughes, M. Kopach, G. Moine, P. Richardson, F. Roschangar, A. Steven, F. Weiberth   +13 more
semanticscholar   +1 more source

Targeting EZH2 reverses thyroid cell dedifferentiation and enhances iodide uptake in anaplastic thyroid cancer

FEBS Letters, EarlyView.
Anaplastic thyroid cancer (ATC) lacks iodide uptake ability due to MAPK activation increasing the expression of the histone methyltransferase EZH2, which represses thyroid differentiation genes (TDGs) such as the sodium iodide symporter (NIS). Dual inhibition of MAPK (U0126) and EZH2 (EPZ6438/Tazemetostat) reverses this mechanism, thus restoring TDG ...
Diego Claro de Mello, Marcella Maringolo Cristovão, Guilherme Henrique, Vinicius Gonçalves Rodrigues, Caroline Serrano‐Nascimento, Edna Teruko Kimura, Cesar Seigi Fuziwara   +6 more
wiley   +1 more source

Coumarin derivatives as acetyl- and butyrylcholinestrase inhibitors: An in vitro, molecular docking, and molecular dynamics simulations study

Heliyon, 2019
Alzheimer's disease is an irreversible and progressive brain disease that can cause problems with memory and thinking skills. It is characterized by loss of cognitive ability and severe behavioral abnormalities, and could lead to death.
Marwa N. Abu-Aisheh, Amal Al-Aboudi, Mohammad S. Mustafa, Mustafa M. El-Abadelah, Saman Yousuf Ali, Zaheer Ul-Haq, Mohammad S. Mubarak   +6 more
doaj   +1 more source

Circulating tumor DNA monitoring and blood tumor mutational burden in patients with metastatic solid tumors treated with atezolizumab

Molecular Oncology, EarlyView.
In patients treated with atezolizumab as a part of the MyPathway (NCT02091141) trial, pre‐treatment ctDNA tumor fraction at high levels was associated with poor outcomes (radiographic response, progression‐free survival, and overall survival) but better sensitivity for blood tumor mutational burden (bTMB).
Charles Swanton, Russell W. Madison, Candice Francheska B. Tambaoan, Funda Meric‐Bernstam, Christopher J. Sweeney, Razelle Kurzrock, Howard A. Burris III, David R. Spigel, Hanna Tukachinsky, Jason Hughes, Julia Malato, Bongin Yoo, Tania Szado, Cheryl Schwab, Lincoln W. Pasquina, Amaya Gasco, Katja Schulze, Claire F. Friedman   +17 more
wiley   +1 more source

Extraction of atenolol from spiked blood serum using a molecularly imprinted polymer sorbent obtained by precipitation polymerization

Heliyon, 2019
Atenolol (ATE) is a cardio-selective β-blocker that is used in the treatment of hypertension over extended periods. However, ATE, like propranolol, has major potential for misuse as a performance-enhancing drug in several sports.
Aliya Nur Hasanah, Driyanti Rahayu, Rimadani Pratiwi, Tina Rostinawati, Sandra Megantara, Febrina Amelia Saputri, Khanifa Hidayati Puspanegara   +6 more
doaj   +1 more source

Molecular imaging predicts trastuzumab‐deruxtecan (T‐DXd) response in head and neck cancer xenograft models

Molecular Oncology, EarlyView.
Trastuzumab‐deruxtecan, a HER2‐targeting antibody‐drug conjugate, shows promising antitumor activity in head and neck squamous cell carcinoma with low HER2 expression. In vitro and in vivo studies demonstrated dose‐dependent cell death and tumor growth reduction in low HER2‐expressing cell lines, which correlated with drug accumulation measured using a
Abdullah Bin Naveed, Lucas Mani, Muhammad Bilal Mirza, Ashtyn McAdoo, Takahito Kondo, Hidenori Tanaka, Nicole Meeks, Eben Rosenthal, Marisa Hom   +8 more
wiley   +1 more source

Glucosamine/L-lactide copolymers as potential carriers for the development of a sustained rifampicin release system using Mycobacterium smegmatis as a tuberculosis model

Heliyon, 2019
The present study aims at developing a new, ultrafine particle-based efficient antibiotic delivery system for the treatment of tuberculosis. The carrier material to make the rifampicin (RIF)-loaded particles is a low molecular weight star-shaped polymer ...
Jorge Ragusa, Daniela Gonzalez, Sumin Li, Sandra Noriega, Maciej Skotak, Gustavo Larsen   +5 more
doaj   +1 more source