Results 41 to 50 of about 73,102 (302)

Brain Delivery of Thyrotropin-Releasing Hormone via a Novel Prodrug Approach

Pharmaceutics, 2019
Using thyrotropin-releasing hormone (TRH) as a model, we explored whether synergistic combination of lipoamino acid(s) and a linker cleaved by prolyl oligopeptidase (POP) can be used as a promoiety for prodrug design for the preferential brain delivery ...
Katalin Prokai-Tatrai, Daniel L. De La Cruz, Vien Nguyen, Benjamin P. Ross, Istvan Toth, Laszlo Prokai   +5 more
doaj   +1 more source

Safety, pharmacokinetic, and efficacy studies of oral DB868 in a first stage vervet monkey model of human African trypanosomiasis [PDF]

, 2013
There are no oral drugs for human African trypanosomiasis (HAT, sleeping sickness). A successful oral drug would have the potential to reduce or eliminate the need for patient hospitalization, thus reducing healthcare costs of HAT.
Arlene S. Bridges (301008), Shelley Ching, Bridges, Arlene S., Raymond E Mdachi, Brun Reto, Wang Michael Zhuo, Wang, Michael Zhuo, Wolf, Kristina K., Ching, Shelley, Arlene S Bridges, Mutuku James N., Murilla, Grace A., Paine, Mary F., Boykin, David W., James N Mutuku, Richard R Tidwell, Mohamed A Ismail, John K. Thuita (148377), Liu, Qiang, Tidwell, Richard R., Hall, James E., Mary F. Paine (148396), John K Thuita, Bridges Arlene S., Ismail Mohamed A., Mdachi, Raymond E., Qiang Liu (166143), Mdachi Raymond E., David W. Boykin (148406), Reto Brun, Reto Brun (41511), Ching Shelley, Hall, James Edwin, Shelley Ching (148404), Tidwell Richard R., Chen, Yao, Mohamed A. Ismail (418629), Boykin David W., Mutuku, James N., James Edwin Hall, Qiang Liu, Grace A Murilla, Hall James Edwin, Raymond E. Mdachi (148398), Mary F Paine, Liu Qiang, Kristina K. Wolf (418627), Michael Zhuo Wang, Thutia, John K., David W Boykin, Yao Chen (149006), Grace A. Murilla (148401), Ismail, Mohamed A., Michael Zhuo Wang (418631), Murilla Grace A., Wolf Kristina K., Kristina K Wolf, James Edwin Hall (418630), Thuita John K., James N. Mutuku (418628), Brun, Reto, Yao Chen, Thuita, John K., Richard R. Tidwell (148409), Paine Mary F., Chen Yao   +65 more
core   +2 more sources

Artificial Intelligence‐Guided Phenotypic Drug Repurposing Against Streptococcus pneumoniae

Advanced Science, EarlyView.
Integrated artificial intelligence (AI) ensembles identify highly potent repurposed drugs against Streptococcus pneumoniae. Prospective virtual screening of 6747 drugs uncovers nine active candidates, including thiostrepton. This drug exhibits low picomolar potency and bypasses established resistance in multidrug‐resistant strains, demonstrating an ...
Joshua S. Fitch, Muhammad D. Ariadi, Min Jung Kwun, Leonie Howells, Saiveth Hernandez‐Hernandez, Nicholas J. Croucher, Pedro J. Ballester   +6 more
wiley   +1 more source

Studies Towards a pH-Sensitive Anticancer Prodrug Model [PDF]

, 2010
Tumour-activated prodrug (TAP) is designed to aim at increasing the prodrug selectivity to kill cancer cells. One strategy to is to design a TAP containing an amine cytotoxin, present as an amide function, which could be released more rapidly in the low ...
Teng, Xiao Shi
core  

Chemical Bond‐Orchestrated Energy Depletion to Augment Lung Cancer Chemo‐Immunotherapy

Advanced Science, EarlyView.
This study grafted dichloroacetic acid (DCA) into perylenediimide (PDI) skeleton via ionic or covalent bond to create novel metabolic agent PDIC‐AC and PDIC‐NAC, explicitly elaborated the underlying energy metabolism and therapeutic mechanism, and developed a promising strategy for energy metabolism‐targeting chemo‐immunotherapy by chemical bond ...
Xuejie Zhao, Yuting Liu, Xiao Huang, Liwen Zhao, Chunli Li, Yongwei Huang   +5 more
wiley   +1 more source

Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir

Nature Communications, 2021
Here, the authors provide a mechanism for an improved version of a nanoformulated myristoylated prodrug of cabotegravir (CAB), named NM2CAB, and its bioavailability, stability and pharmacokinetics in mice and rats performed in independent academic and a ...
Nagsen Gautam, JoEllyn M. McMillan, Devendra Kumar, Aditya N. Bade, Qiaoyu Pan, Tanmay A. Kulkarni, Wenkuan Li, Brady Sillman, Nathan A. Smith, Bhagya L. Dyavar Shetty, Adam Szlachetka, Benson J. Edagwa, Howard E. Gendelman, Yazen Alnouti   +13 more
doaj   +1 more source

Conditions for safe and effective ADEPT treatment [PDF]

, 2010
Antibody directed enzyme prodrug therapy (ADEPT) is a drug delivery system developed for the treatment of cancer. ADEPT uses a systemically administered antibody, tethered to an enzyme, to localize enzyme in tumour deposits.
Wilkins, D.K.
core  

Overcoming Drug Resistance by Paclitaxel Resistance in Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
In the murine triple‐negative breast cancer (TNBC) model, chemotherapy effectively increases tumor neoantigen burden (TNB). Here, the study constructs a liposomal nanovaccine using antigens derived from in vitro chemotherapy‐treated paclitaxel‐resistant TNBC 4T1 cells.
Bo Chen, Yangyi Wang, Tingting Li, Changqing Guo, Zhe Xie, Zhixian Zhang, Xinghua Han, Wei Wang, Jian Wang, Xiaopeng Ma, Yuanzeng Min   +10 more
wiley   +1 more source

Structural insights into catalytical capability for CPT11 hydrolysis and substrate specificity of a novel marine microbial carboxylesterase, E93

Frontiers in Microbiology, 2023
IntroductionCPT11 (Irinotecan; 7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin) is an important camptothecin-based broad-spectrum anticancer prodrug.
Yang Li, Yang Li, Zhen Rong, Zhengyang Li, Henglin Cui, Jixi Li, Xue-Wei Xu   +6 more
doaj   +1 more source

pH Sensitive Anticancer Prodrug: Amide of Kemp's Acid [PDF]

, 2009
Solid tumours are characterised by lower extracellular pH (as low as 5.8 pH) compared to normal healthy cellular pH (actively regulated at pH 7.3). This difference may be exploited with an acid-sensitive anti-tumour prodrug which releases a cytotoxin ...
Brooks, Robert Turongo
core