Results 61 to 70 of about 9,364,265 (259)

In vitro and in silico modelling of ROS1‐positive non‐small cell lung cancer reveals fusion‐dependent tyrosine kinase inhibitor responses

Molecular Oncology, EarlyView.
Drug resistance limits treatment success in a subset of lung cancers driven by ROS1 gene alterations. Using patient‐derived cells and computer simulations, we studied three key mutations and how they affect five targeted drugs. The mutations reduced drug effectiveness in different ways by altering protein structure and behavior.
Farhan Ul Haq, Marc Terrones, Felicia Rodrigues Fortes, Anne Schepers, Alessia Denis, Christophe Deben, Ken Op de Beeck, Guy Van Camp, Geert Vandeweyer   +8 more
wiley   +1 more source

Electronic and Steric Effects Control Regioselectivity in Alkyne Migratory Insertion during Ni-Catalyzed Indenone Synthesis

, 2023
Many useful transition-metal-catalyzed reactions depend on the migratory insertion of an alkyne into a metal–carbon bond. Steric effects, electronic effects, and coordinating directing groups have all been shown to control product distributions in ...
Logan M. Whitt (14657791), Lydia P. Moore (14657782), Mei Lin N. Dye (12210763), Zachary J. Hagedorn (14657785), Dale J. Wilger (2028226), Megan E. Barnes (14657788)   +5 more
core   +1 more source

Paclitaxel induces NM2‐dependent cellular contraction through GEF‐H1 dissociation from microtubules and RhoA/ROCK activation in cancer cells

Molecular Oncology, EarlyView.
Taxanes are widely used chemotherapeutics whose effects on cellular mechanics remain poorly understood. We show that paclitaxel induces rapid cellular contraction by promoting GEF‐H1 dissociation from microtubules and non‐muscle myosin II activation through RhoA/ROCK.
Gloria Asensio‐Juárez, Rafael Pérez‐Díaz, Hugo Ramos‐Solano, Marina Garrido‐Casado, Vanessa C. Talayero, Miguel Vicente‐Manzanares   +5 more
wiley   +1 more source

Steric Effects in the Reaction of Aryl Radicals on Surfaces

, 2016
Steric effects are investigated in the reaction of aryl radicals with surfaces. The electrochemical reduction of 2-, 3-, 4-methyl, 2-methoxy, 2-ethyl, 2,6-, 2,4-, and 3,5-dimethyl, 4-tert-butyl, 3,5-bis-tert-butyl benzenediazonium, 3,5-bis ...
Catherine Combellas (1431925), De-en Jiang (1270428), Frédéric Kanoufi (1431916), Jean Pinson (1431919), Fetah I. Podvorica (1674043)   +4 more
core   +1 more source

Mutant p53R273H disrupts PDPK1 homodimerization and contributes to PDPK1 activation

Molecular Oncology, EarlyView.
How mutant p53R273H drives AKT signaling is unclear. We show that p53R273H, but not wild‐type, directly binds PDPK1 via a mutation‐dependent conformational change. This interaction disrupts inhibitory PDPK1 homodimerization and enhances AKT phosphorylation.
Mei Chee Lim, Alvin Kunyao Guo, Yoko Itahana, Srinivasaraghavan Kannan, Valerie Goh, Mingmin Ong, Terina Yan Wen Tay, Weiying Ye, Sabhashina Radha Krishnan, Jun Nishiyama, Chandra S Verma, Koji Itahana   +11 more
wiley   +1 more source

Semiempirical and Ab Initio calculation of the molecular structures of substituted N-Benzoylimidazoles

Semina: Ciências Exatas e Tecnológicas, 2001
Possible reasons of low reactivities of some N-(2-X-benzoyl) imidazoles utilising ab initio Hartree-Fock calculations have been studied in imidazole-catalyzed hydrolysis.
Paulo Meneghelli
doaj  

Conformation and Steric Effects in Mono- and Dimethoxybenzoic Acids

, 2016
The conformation of mono- and dimethoxybenzoic acids in solution was determined from their IR spectra and 13C and 1H NMR spectra. The main feature is a strong intramolecular hydrogen bond in all 2-methoxy derivatives that persists even in polar aprotic ...
Miloš Buděšínský (2454460), Otto Exner (2277745), Jiří Kulhánek (3046968), Pavel Fiedler (2175678)   +3 more
core   +1 more source

Structural studies and functional engineering of NanX: an anhydro‐sialic acid transporter from Escherichia coli

FEBS Open Bio, EarlyView.
Biophysical characterisation shows that NanX, a membrane transport protein from the major facilitator superfamily (MFS), forms both monomers and dimers after purification. AlphaFold modelling and substrate docking provide information on residues likely involved in substrate recognition for NanX and another MFS member, NanT.
Michael C. Newton‐Vesty, Kelsi R. Hall, Zachary D. Tillett, Liam S. Turk, James S. Davies, Michael J. Currie, Hamish G. Brown, Sepideh Valimehr, Peter D. Mace, Andrew E. Whitten, Santosh Panjikar, Eric Hanssen, Rachel A. North, Renwick C.J. Dobson   +13 more
wiley   +1 more source

(How) does 1,3,5-triethylbenzene scaffolding work? Analyzing the abilities of 1,3,5-triethylbenzene- and 1,3,5-trimethylbenzene-based scaffolds to preorganize the binding elements of supramolecular hosts and to improve binding of targets

Beilstein Journal of Organic Chemistry, 2012
1,3,5-triethylbenzenes have been widely used as supramolecular templates to organize molecular-recognition elements. It is believed that the steric-gearing effect of the 1,3,5-triethylbenzene template directs the binding elements toward the same face of ...
Xing Wang, Fraser Hof
doaj   +1 more source

Hydrogen Transfer from Hantzsch 1,4-Dihydropyridines to Carbon-Carbon Double Bonds under Microwave Irradiation

Molecules, 2002
1,4-Dihydropyridines (DHPs) have been used in the reduction of carbon-carbon double bonds under microwave irradiation without solvent. The efficiency of the reactions is dramatically dependent on the steric effects in the DHPs and on the electronic ...
Jean Jacques Vanden Eynde, Didier Barbry, Guy Cordonnier, Séverine Torchy   +3 more
doaj   +1 more source