Results 201 to 210 of about 231,218 (308)

TBC1D15 functions as an Arl4D GAP and promotes the mitochondrial translocation of Arl4D for organelle homeostasis. [PDF]

J Cell Sci
Chen CT, Liu TJ, Lin SJ, Chang TW, Lee FS.   +4 more
europepmc   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Disrupting the KRAS-SOS1 protein-protein interaction: mechanistic rationale for pan-KRAS pathway suppression and combination therapy. [PDF]

Front Chem
Kamel EM, Khadrawy SM, Ali MAM, Abukhadra MR, Yassin NYS, Alkhedhairi S, Aba Alkhayl FF, Lamsabhi AM.   +7 more
europepmc   +1 more source

Therapeutic potential of small molecules that block receptor‐induced Kv7/M‐current suppression in neuroprotection, seizures, and pain

British Journal of Pharmacology, EarlyView.
Receptor‐induced Kv7/M‐current suppression increases neuronal activity and contributes to pathology of several conditions. A new class of Kv7 modulators identified in this study attenuates M‐current suppression and shows therapeutic effects. Abstract Background and Purpose Neuronal Kv7 channels generate low voltage–gated potassium currents known as the
Young Woo Kim, Pavan Kumar Behara, Lamees Alhassen, Cindy Wong, Olivier Civelli, Naoto Hoshi   +5 more
wiley   +1 more source

Identification of Small-Molecule Inhibitors that Block the GTP-Binding Pocket of K-Ras and Other Members of the Ras Superfamily of Small GTPases. [PDF]

Mol Cancer Ther
Carta L, Hutcheson R, Bigarella CL, Zhang S, Davis SA, Rudolph MJ, Reynolds CH, Quick M, Williams TM, Schmertzler M, Hadari YR.   +10 more
europepmc   +1 more source

Cardiotoxicity of BRAF/MEK inhibitors

British Journal of Pharmacology, EarlyView.
Abstract Rapidly accelerated fibrosarcoma type B/B‐Raf proto‐oncogene, serine/threonine kinase (BRAF) and mitogen‐activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real‐world clinical practice.
Katharina Seuthe, Valerie Lohner, Kevin Terre, Thomas Riffelmacher, Roman Pfister   +4 more
wiley   +1 more source

Structures and mechanism of E2-CBASS anti-phage system. [PDF]

mLife
Xiao J, Yan Y, Li J, Oyejobi GK, Lan D, Zhu B, Wang Z, Wang L.   +7 more
europepmc   +1 more source

Memantine prevents acute stress‐induced memory deficits by reversing sex‐dependent pathophysiological glutamatergic alterations in the dorsal hippocampus

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The neural mechanisms underlying effects of acute stress on memory are poorly understood. We demonstrated previously that acute stress produces identical spatial memory deficits in male and female mice but through distinct molecular mechanisms, with females exhibiting up‐regulation of N‐methyl‐D‐aspartate (NMDA) receptor
Sebastiano A. Torrisi, Lidia Diolosà, Giuseppe Aceto, Claudia Marchetti, Federica Geraci, Konstantinos Partsinevelos, Silvia Rizzo, Margherita Grasso, Filippo Caraci, Francesco Bellia, Giovanni Li Volti, Angela Maria Amorini, Marcello D′Ascenzo, Gian Marco Leggio   +13 more
wiley   +1 more source

The Role of the TG2-GPR56 Complex in Cutaneous Squamous Cell Carcinoma (CSCC) Aggression and Therapeutic Resistance. [PDF]

Int J Mol Sci
Weber DJ, Cook ME, Yu W, Redondo M, Godoy-Ruiz R.   +4 more
europepmc   +1 more source

Shared and specific molecular mechanisms of proteasome inhibitors in chemotherapy‐induced peripheral neurotoxicity

British Journal of Pharmacology, EarlyView.
This study compares the molecular mechanisms of chemotherapy‐related peripheral neurotoxicity of two proteasome inhibitors, bortezomib and carfilzomib, using a multidisciplinary approach to reveal that, alongside shared effects on mitochondria structure and function, the more neurotoxic drug BTZ has specific effects on microtubules and mitochondrial ...
Federico Iseppon, Alessio Malacrida, Alessia Chiorazzi, Annalisa Canta, Paola Alberti, Valentina Alda Carozzi, Eleonora Pozzi, Virginia Rodriguez‐Menendez, Laura Cherchi, Valentina Fabbro, Lisa Pagani, Elisa Tonelli, Laura Tapella, Andrea Mattarei, Sara Palermo, Daniele Cartelli, Mario Mauri, Noemi Scimia, Serena Stanga, Dmitry Lim, Carla Distasi, Marta Delconti, Clizia Chinello, Patricia Morcillo, Maria Elena Pero, Francesca Bartolini, Guido Cavaletti, Cristina Meregalli   +27 more
wiley   +1 more source