Results 81 to 90 of about 107,657 (326)

Cell geometry and membrane protein crowding constrain Escherichia coli growth rate, overflow metabolism, respiration, and maintenance energy

FEBS Letters, EarlyView.
The physical dimensions and shape of bacterial cells define the surface area available to acquire nutrients and the volume available for synthesizing proteins and DNA. Here, we use computational systems biology to decode the importance of cell geometry as a major determinant of prokaryotic phenotype, including growth rate and metabolic efficiency. This
Ross P. Carlson, Tomáš Gedeon, Mauricio Garcia Benitez, Campbell Putnam, William R. Harcombe, Radhakrishnan Mahadevan, Ashley E. Beck   +6 more
wiley   +1 more source

The plasma membrane as a competitive inhibitor and positive allosteric modulator of KRas4B signaling

bioRxiv, 2019
Mutant Ras proteins are important drivers of human cancers, yet no approved drugs act directly on this difficult target. Over the last decade, the idea has emerged that oncogenic signaling can be diminished by molecules that drive Ras into orientations ...
Chris Neale, A. Garcia
semanticscholar   +1 more source

To Inhibit or Enhance? Is There a Benefit to Positive Allosteric Modulation of P2X Receptors? [PDF]

Frontiers in Pharmacology, 2020
The family of ligand-gated ion channels known as P2X receptors were discovered several decades ago. Since the cloning of the seven P2X receptors (P2X1-P2X7), a huge research effort has elucidated their roles in regulating a range of physiological and pathophysiological processes.
Stokes, Leanne, Bidula, Stefan, Bibič, Lučka, Allum, Elizabeth   +3 more
openaire   +5 more sources

GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models

, 2010
Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for treatment of seizures and epilepsy. Previous studies have shown that the endogenous peptide ligand galanin exerts powerful anticonvulsant ...
Roger Baldwin, Tianyu Liu, Fengcheng Xia, Xiaoying Lu, Edward Roberts, Manuel Sanchez-Alavez, Claude G. Wasterlain, James Chang, Stephanie Wu, Tamas Bartfai   +9 more
core   +1 more source

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

Molecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

Distinct potency of compounds targeting the T1R3 subunit in modulating the response of human sweet and umami taste receptors

Scientific Reports
The heterodimeric G-protein-coupled receptors T1R2/T1R3 and T1R1/T1R3 have been identified as sweet and umami taste receptors, respectively, and both of these receptors share the T1R3 subunit.
Maiko Kawasaki, Yuta Kidera, Ryusei Goda, Chiaki Taketani, Misato Ide, Wataru Fujii, Tomoya Nakagita, Takumi Misaka   +7 more
doaj   +1 more source

Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine [v1; ref status: indexed, http://f1000r.es/o0]

F1000Research, 2013
We investigated the role of metabotropic glutamate receptor type 5 (mGluR5) in methamphetamine-induced behavioral sensitization. The mGluR5 positive allosteric modulator (3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamide (CDPPB) and negative allosteric ...
Peter R Kufahl, Natali E Nemirovsky, Lucas R Watterson, Nicholas Zautra, M Foster Olive   +4 more
doaj   +1 more source

Conformational diversity in class C GPCR positive allosteric modulation

Nature Communications, 2023
Abstract The metabotropic glutamate receptors (mGlus) are class C G protein coupled receptors (GPCR) that form obligate dimers activated by the major excitatory neurotransmitter L-glutamate 1,2 . The architecture of mGlu receptor comprises an extracellular Venus-Fly Trap domain (VFT)
Giuseppe Cannone, Ludovic Berto, Fanny Malhaire, Gavin Ferguson, Aurelien Fouillen, Stéphanie Balor, Joan Font-Ingles, Amadeu Llebaria, Cyril Goudet, Abhay Kotecha, Vinothkumar K.R., Guillaume Lebon   +11 more
openaire   +4 more sources

Hippo pathway at the crossroads of stemness and therapeutic resistance in breast cancer

Molecular Oncology, EarlyView.
Dysregulation of the Hippo pathway drives nuclear accumulation of YAP/TAZ, activating stemness‐related transcriptional programs that sustain breast cancer stemness and fuel therapeutic resistance across subtypes, underscoring Hippo signaling as a targetable vulnerability. Figure created and edited with BioRender.com.
Giulia Schiavoni, Antonella Palmese, Stefano Scalera, Laura Cipriani, Davide Mascolo, Patrizia Vici, Teresa Arcuri, Lorena Filomeno, Eriseld Krasniqi, Giovanni Blandino, Giulia Bon, Marcello Maugeri‐Saccà   +11 more
wiley   +1 more source

Galantamine is not a positive allosteric modulator of human α4β2 or α7 nicotinic acetylcholine receptors

British Journal of Pharmacology, 2018
The alkaloid galantamine was originally isolated from the green snowdrop Galanthus woronowii and is currently marketed as a drug for treatment of mild to moderate dementia in patients with Alzheimer's disease. In addition to a well‐documented proficiency
N. M. Kowal, P. Ahring, V. Liao, Dinesh C Indurti, Benjamin S. Harvey, S. O'Connor, M. Chebib, E. Olafsdottir, T. Balle   +8 more
semanticscholar   +1 more source