Results 1 to 10 of about 2,059 (202)

Alpha Ketoglutarate Downregulates the Neutral Endopeptidase and Enhances the Growth Inhibitory Activity of Thiorphan in Highly Aggressive Osteosarcoma Cells [PDF]

Molecules, 2022
Since natural substances are widely explored as epigenetic modulators of gene expression and epigenetic abnormalities are important causes of cancerogenesis, factors with pro-tumor activities subjected to epigenetic control, e.g., neutral endopeptidase ...
Magdalena Mizerska-Kowalska, Adrianna Sławińska-Brych, Emilia Niedziela, Viktor Brodovskiy, Barbara Zdzisińska   +4 more
doaj   +4 more sources

Evaluation of In-Batch and In-Flow Synthetic Strategies towards the Stereoselective Synthesis of a Fluorinated Analogue of Retro-Thiorphan [PDF]

Molecules, 2019
A stereoselective synthetic strategy for the preparation of trifluoromethylamine mimics of retro-thiorphan, involving a diastereoselective, metal-free catalytic step, has been studied in batch and afforded the target molecule in good yields and high ...
Margherita Pirola, Alessandra Puglisi, Laura Raimondi, Alessandra Forni, Maurizio Benaglia   +4 more
doaj   +4 more sources

Integrating metabolomics, bionics, and culturomics to study probiotics-driven drug metabolism [PDF]

Frontiers in Pharmacology, 2023
Many drugs have been shown to be metabolized by the human gut microbiome, but probiotic-driven drug-metabolizing capacity is rarely explored. Here, we developed an integrated metabolomics, culturomics, and bionics framework for systematically studying ...
Bohai Li, Bohai Li, Bohai Li, Lai-Yu Kwok, Lai-Yu Kwok, Lai-Yu Kwok, Dandan Wang, Dandan Wang, Dandan Wang, Lu Li, Lu Li, Lu Li, Shuai Guo, Shuai Guo, Shuai Guo, Yongfu Chen, Yongfu Chen, Yongfu Chen   +17 more
doaj   +2 more sources

CRISPR/Cas9-engineering of Kell null erythrocytes to unveil host targeted irresistible antimalarial [PDF]

Communications Biology
Malaria elimination faces challenges from drug resistance, stemming from mutations within the parasite’s genetic makeup. Genetic adaptations in key erythrocyte proteins offer malaria protection in endemic regions.
Geeta Kumari, Pragya Gupta, Sangam G. Goswami, Ravi Jain, Sakshi Anand, Shreeja Biswas, Swati Garg, Priya Thakur, Vinodh Saravanakumar, V. R. Arvinden, Bidhan Goswami, Ipsita Pal Bhowmick, Narla Mohandas, Jeremy Burrows, Sivaprakash Ramalingam, Shailja Singh   +15 more
doaj   +2 more sources

Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity [PDF]

Biomedicines, 2021
Background: Alzheimer’s disease (AD) involves impairment of Aβ clearance. Neprilysin (NEP) is the most efficient Aβ peptidase. Enhancement of the activity or expression of NEP may provide a prominent therapeutic strategy against AD.
Dimitris Matiadis, See-Ting Ng, Eric H.-L. Chen, Georgia Nigianni, Veroniki P. Vidali, Aleksander Canko, Rita P.-Y. Chen, Marina Sagnou   +7 more
doaj   +2 more sources

Exploiting the angiotensin-converting enzyme pathway to augment endogenous opioid signaling [PDF]

Communications Biology
Angiotensin Converting Enzyme (ACE) impacts hemodynamics by regulating the conversion of angiotensin I to the vasoconstricting angiotensin II. We recently identified a non-canonical central role of ACE in the degradation of enkephalin heptapeptide, Met ...
Prakashkumar Dobariya, Jessica Williams, Filip Hanak, Patrick E. Rothwell, Swati S. More   +4 more
doaj   +2 more sources

A comprehensive review of the pharmacodynamics, pharmacokinetics and clinical effects of the neutral endopeptidase inhibitor racecadotril [PDF]

Frontiers in Pharmacology, 2012
Racecadotril, via its active metabolite thiorphan, is an inhibitor of the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), thereby increasing exposure to NEP including enkephalins and atrial natriuretic peptide.
Marion eEberlin, Thomas eMück, Martin C Michel   +2 more
doaj   +5 more sources

Exogenous Angiotensin I Metabolism in Aorta Isolated from Streptozotocin Treated Diabetic Rats [PDF]

Journal of Diabetes Research, 2016
Purpose. Products of angiotensin (ANG) I metabolism may predispose to vascular complications of diabetes mellitus. Methods. Diabetes was induced with streptozotocin (75 mg/kg i.p.).
P. P. Wołkow, B. Bujak-Giżycka, J. Jawień, R. Olszanecki, J. Madej, J. Rutowski, R. Korbut   +6 more
doaj   +2 more sources

Significance of CD10 for Mucosal Immunomodulation by β-Casomorphin-7 in Exacerbation of Ulcerative Colitis [PDF]

Current Issues in Molecular Biology
β-Casomorphin-7 (BCM), a breakdown product of milk β-casein, exhibits opioid activity. Opioids are known to affect the immune system, but the effects of BCM on ulcerative colitis (UC) are not clear.
Yoshihiro Miyagawa, Rina Fujiwara-Tani, Ayaka Ikemoto, Rika Sasaki, Ruiko Ogata, Yukiko Nishiguchi, Kei Goto, Isao Kawahara, Takamitsu Sasaki, Hiroki Kuniyasu   +9 more
doaj   +2 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