Results 81 to 90 of about 396,504 (303)

Plecstatin inhibits hepatocellular carcinoma tumorigenesis and invasion through cytolinker plectin

Molecular Oncology, EarlyView.
The ruthenium‐based metallodrug plecstatin exerts its anticancer effect in hepatocellular carcinoma (HCC) primarily through selective targeting of plectin. By disrupting plectin‐mediated cytoskeletal organization, plecstatin inhibits anchorage‐dependent growth, cell polarization, and tumor cell dissemination.
Zuzana Outla, Jan Kosla, Magdalena Prechova, Lukas Frick, Patricia Bortel, Yasmin Borutzki, Andrea Bileck, Christopher Gerner, Samuel M. Meier‐Menches, Selma Osmanagic‐Myers, Martin Gregor   +10 more
wiley   +1 more source

Drug-bound outward-facing conformation of a heterodimeric ABC exporter suggests a putative mechanism of drug translocation

Nature Communications
Multidrug transport by ATP binding cassette (ABC) exporters entails a mechanism to modulate drug affinity across the transport cycle. Here, we combine cryo-EM and molecular dynamics (MD) simulations to illuminate a lipid-competition mechanism to drive ...
Qingyu Tang, Matt Sinclair, Paola Bisignano, Yunsen Zhang, Emad Tajkhorshid, Hassane S. Mchaourab   +5 more
doaj   +1 more source

Dynamics of ABC Transporter P-glycoprotein in Three Conformational States. [PDF]

, 2019
We used hydrogen-deuterium exchange mass spectrometry (HDX-MS) to obtain a comprehensive view of transporter dynamics (85.8% sequence coverage) occurring throughout the multidrug efflux transporter P-glycoprotein (P-gp) in three distinct conformational ...
Chang, Geoffrey, Komives, Elizabeth A, Kopcho, Noah   +2 more
core   +1 more source

Inhibitor binding mode and allosteric regulation of Na+-glucose symporters. [PDF]

, 2018
Sodium-dependent glucose transporters (SGLTs) exploit sodium gradients to transport sugars across the plasma membrane. Due to their role in renal sugar reabsorption, SGLTs are targets for the treatment of type 2 diabetes.
Althoff, Thorsten, Bisignano, Paola, Friemann, Rosmarie, Ghezzi, Chiara, Grabe, Michael, Jacobson, Matthew P, Jo, Hyunil, Kalyanaraman, Chakrapani, Polizzi, Nicholas F, Wright, Ernest M   +9 more
core   +2 more sources

Therapeutic strategies for MMAE‐resistant bladder cancer through DPP4 inhibition

Molecular Oncology, EarlyView.
We established monomethyl auristatin E (MMAE)‐resistant bladder cancer (BC) cell lines by exposure to progressively increasing concentrations of MMAE in vitro. RNA sequencing showed DPP4 expression was increased in MMAE‐resistant BC cells. Both si‐DPP4 and the DPP4 inhibitor sitagliptin suppressed the viability of MMAE‐resistant BC cells.
Gang Li, Shuichi Tatarano, Hirofumi Yoshino, Saeki Saito, Mitsuhiko Tominaga, Junya Arima, Ikumi Fukuda, Takashi Sakaguchi, Ryosuke Matsushita, Yasutoshi Yamada, Hideki Enokida   +10 more
wiley   +1 more source

Fluoxetine: a case history of its discovery and preclinical development [PDF]

, 2014
Introduction: Depression is a multifactorial mood disorder with a high prevalence worldwide. Until now, treatments for depression have focused on the inhibition of monoaminergic reuptake sites, which augment the bioavailability of monoamines in the CNS ...
Bel N, Bergstrom RF, Bravo L, Bremner JD, Burrows GD, Chouinard G, Datla KP, Esther Berrocoso, Juan Antonio Mico, Kreiss DS, Laura Perez-Caballero, Lemberger L, Li Q, Lidia Bravo, Maj J, Nibuya M, Owens MJ, Rutter JJ, Sonia Torres-Sanchez, Stevens JC, Wong DT   +20 more
core   +2 more sources

Dammarenediol II enhances etoposide‐induced apoptosis by targeting O‐GlcNAc transferase and Akt/GSK3β/mTOR signaling in liver cancer

Molecular Oncology, EarlyView.
Etoposide induces DNA damage, activating p53‐dependent apoptosis via caspase‐3/7, which cleaves PARP1. Dammarenediol II enhances this apoptotic pathway by suppressing O‐GlcNAc transferase activity, further decreasing O‐GlcNAcylation. The reduction in O‐GlcNAc levels boosts p53‐driven apoptosis and influences the Akt/GSK3β/mTOR signaling pathway ...
Jaehoon Lee, Byung‐Cheol Han, Gi‐Bang Koo, Jihye Park, Mijin Kwon, Young Bin Park, Jae‐Mun Choi, Seung‐Ho Lee, Sangho Roh   +8 more
wiley   +1 more source

Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment

Molecular Oncology, EarlyView.
This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley   +1 more source

Gellan Gum Promotes the Differentiation of Enterocytes from Human Induced Pluripotent Stem Cells

Pharmaceutics, 2020
The evaluation of drug pharmacokinetics in the small intestine is critical for developing orally administered drugs. Caucasian colon adenocarcinoma (Caco-2) cells are employed to evaluate drug absorption in preclinical trials of drug development. However,
Shimeng Qiu, Tomoki Kabeya, Isamu Ogawa, Shiho Anno, Hisato Hayashi, Tatsuro Kanaki, Tadahiro Hashita, Takahiro Iwao, Tamihide Matsunaga   +8 more
doaj   +1 more source

Not only P-glycoprotein: amplification of the ABCB1-containing chromosome region 7q21 confers multidrug resistance upon cancer cells by coordinated overexpression of an assortment of resistance-related proteins [PDF]

, 2017
The development of drug resistance continues to be a dominant hindrance toward curative cancer treatment. Overexpression of a wide-spectrum of ATP-dependent efflux pumps, and in particular of ABCB1 (P-glycoprotein or MDR1) is a well-known resistance ...
Assaraf, Yehuda G., Colotti, Gianni, Fazi, Francesco, Genovese, Ilaria, Ilari, Andrea   +4 more
core   +1 more source