Results 11 to 20 of about 1,836 (178)

Thiorphan reprograms neurons to promote functional recovery after spinal cord injury [PDF]

Nature
Abstract We previously identified an embryonic shift in the corticospinal motor neuronal transcriptome after spinal cord injury associated with successful axonal regeneration 1 .
Erna Van Niekerk, Mark H Tuszynski
exaly   +3 more sources

Opioid Withdrawal Abruptly Disrupts Amygdala Circuit Function by Reducing Peptide Actions. [PDF]

J Neurosci, 2023
While the physical signs of opioid withdrawal are most readily observable, withdrawal insidiously drives relapse and contributes to compulsive drug use, by disrupting emotional learning circuits.
Gregoriou GC, Patel SD, Pyne S, Winters BL, Bagley EE.   +4 more
europepmc   +3 more sources

Pharmacophore-Based Identification and Molecular Characterization of Potent Neprilysin Inhibitors: Biochemical and Therapeutic Implications for Cardiovascular Diseases. [PDF]

Chem Biol Drug Des
Pharmacophore‐based virtual screening and molecular dynamics identified pentagalloylglucose and tannic acid as potent, non‐toxic neprilysin inhibitors. These natural compounds demonstrated strong binding affinity and stable interactions with the catalytic Zn2+ site, offering promising leads for cardiovascular drug development. ABSTRACT Neprilysin (NEP),
Kuo CT, Wu YC, Li JM, Ju TC, Tseng TS.
europepmc   +2 more sources

Thiorphan and retro-thiorphan display equivalent interactions when bound to crystalline thermolysin [PDF]

Biochemistry, 1989
The three-dimensional structures of (S)-thiorphan and (R)-retro-thiorphan bound to thermolysin have been determined crystallographically and refined to residuals of 0.183 and 0.187 at 1.7-A resolution. Thiorphan [N-[(S)-2-(mercaptomethyl)-1-oxo-3-phenylpropyl]glycine] [HSCH2CH(CH2C6H5)CONHC-H2COOH] and retro-thiorphan [[[(R)-1-(mercaptomethyl)-2 ...
S L, Roderick, M C, Fournie-Zaluski, B P, Roques, B W, Matthews   +3 more
  +6 more sources

Ligand Screening and Discovery Using Cocktail Soaking and Automated Microcrystal Electron Diffraction. [PDF]

ChemMedChem
Cocktail soaking using single‐crystal X‐ray diffraction allows high‐throughput crystallographic ligand screening against protein targets. However, protein microcrystals are not amenable to this approach. Herein, a workflow integrating cocktail soaking with automated microcrystal electron diffraction to allow rapid ligand screening, structure ...
Lin J, Gallenito MJ, Hattne J, Gonen T.
europepmc   +2 more sources

Design, synthesis, and evaluation of novel racecadotril-tetrazole-amino acid derivatives as new potent analgesic agents

Research in Pharmaceutical Sciences, 2021
Background and purpose: Although pain is one of the most common symptoms of diseases, it is often mismanaged due to limited access to painkillers and ineffectiveness, unacceptable side effects, or the possibility of abuse.
Mehdi Asadi, Maryam Mohammadi-Khanaposhtani, Faezeh Sadat Hosseini, Mahdi Gholami, Ahmad Reza Dehpour, Massoud Amanlou   +5 more
doaj   +1 more source

Granulocyte-colony stimulating factor attenuates oligomeric amyloid β neurotoxicity by activation of neprilysin. [PDF]

PLoS ONE, 2014
Soluble oligomeric amyloid β (oAβ) causes synaptic dysfunction and neuronal cell death, which are involved in the pathogenesis of Alzheimer's disease (AD).
Yukiko Doi, Hideyuki Takeuchi, Hiroyuki Mizoguchi, Kazuya Fukumoto, Hiroshi Horiuchi, Shijie Jin, Jun Kawanokuchi, Bijay Parajuli, Yoshifumi Sonobe, Tetsuya Mizuno, Akio Suzumura   +10 more
doaj   +1 more source

Concomitant medication in patients with bradykinin‐mediated angioedema – there's more than ACE inhibitors

JDDG: Journal der Deutschen Dermatologischen Gesellschaft, Volume 21, Issue 11, Page 1283-1289, November 2023., 2023
Summary Bradykinin‐mediated angioedema is a rare, non‐allergic, potentially life‐threatening disease. ACE inhibitor‐induced angioedema and hereditary angioedema (HAE) are the two most common presentations. Therapeutic options, pathophysiology and diagnosis continue to be investigated, with considerable progress in HAE over the last few decades. For all
Robin Lochbaum, Thomas K. Hoffmann, Jens Greve, Janina Hahn   +3 more
wiley   +1 more source

Medikamente als Auslöser Bradykinin‐vermittelter Angioödeme – mehr als ACE‐Hemmer

JDDG: Journal der Deutschen Dermatologischen Gesellschaft, Volume 21, Issue 11, Page 1283-1290, November 2023., 2023
Zusammenfassung Bradykinin‐vermittelte Angioödeme sind seltene, nichtallergische und potenziell lebensbedrohliche Krankheiten. Die beiden bekanntesten Formen sind das ACE‐Hemmer‐induzierte Angioödem und das hereditäre Angioödem (HAE). Die therapeutischen Möglichkeiten, die Pathophysiologie und die Diagnostik werden weiter erforscht, wobei beim HAE in ...
Robin Lochbaum, Thomas K. Hoffmann, Jens Greve, Janina Hahn   +3 more
wiley   +1 more source

The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders

British Journal of Pharmacology, Volume 180, Issue 7, Page 879-893, April 2023., 2023
Despite the increasing impact of opioid use disorders on society, there is a disturbing lack of effective medications for their clinical management. An interesting innovative strategy to treat these disorders consists in the protection of endogenous opioid peptides to activate opioid receptors, avoiding the classical opioid‐like side effects.
Beltran Alvarez‐Perez, Hervé Poras, Rafael Maldonado   +2 more
wiley   +1 more source