Results 91 to 100 of about 206,533 (287)

Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs

Acta Pharmaceutica Sinica B, 2020
In this report, a series of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives were designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket (NNIBP) by incorporating an aromatic ...
Dongwei Kang, Da Feng, Tiziana Ginex, Jinmi Zou, Fenju Wei, Tong Zhao, Boshi Huang, Yanying Sun, Samuel Desta, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu   +12 more
doaj   +1 more source

Innovative Agents for Actinic Keratosis and Nanocarriers Enhancing Skin Penetration [PDF]

, 2010
Actinic keratosis and cutaneous squamous cell carcinoma are of increasing importance with aging and increased ultraviolet light exposure in Western societies. Efficient and well-tolerated therapy is still a matter of concern.
Höltje, H.-D., Höltje, M., Korting, Hans Christian, Schäfer-Korting, Monika   +3 more
core   +1 more source

Ovarian Matrisome Dynamics and αvβ3‐Mediated Regulation in Early Follicular Development

Advanced Science, EarlyView.
The matrisome undergoes dynamic remodeling during early follicular development. Integrin αvβ3 mediates matrisome signals, regulating primordial follicle activation/atresia and secondary follicle growth via Hippo/mTOR pathways, with conserved roles in human ovaries, offering therapeutic targets for ovarian disorders.
Tong Wu, Yanzhi Feng, Qingqing Zhu, Ting Jiang, Yueyue Gao, Kebing Nie, Xianan Tang, Ying Chen, Dianxing Hu, Xudan Yang, Shixuan Wang, Meng Wu, Jinjin Zhang   +12 more
wiley   +1 more source

Drug resistance and viral tropism in HIV-1 subtype C-infected patients in KwaZulu-Natal, South Africa: implications for future treatment options [PDF]

, 2011
Article approval pendingDrug resistance poses a significant challenge for the successful application of highly active antiretroviral therapy (HAART) globally. Furthermore, emergence of HIV-1 isolates that preferentially use CXCR4 as a coreceptor for cell
Ashika Singh, Bjorndal, Brenner, Briggs, Briz, Cann, Cecilia, Cilliers, Coakley, Coetzer, Connor, Cozzi-Lepri, Daniel R. Kuritzkes, Elizabeth D. Anton, Fouchier, Fouchier, Furtado, Henry Sunpath, Hosseinipour, Hunt, Irlbeck, Jacqueline D. Reeves, Johnston, Kantor, Keshni Hiramen, Kuiken, Loemba, Low, Marconi, Nagavelli Padayachi, Ndungu, Novitsky, Reeves, Richard Murphy, Rizzuto, Scarlatti, Singh, Tamura, Taryn N. Green, Taylor, Thumbi Ndung'u, Tobin, Trinh, Tscherning, Wallis, Westby, Whitcomb, Wu, Yolanda Lie   +48 more
core   +2 more sources

Gut Microbiota‐Derived Anandamide Mediates the Therapeutic Effects of Urolithin A on Alcohol‐Induced Cognitive and Social Dysfunction via CB1R‐DRD2‐RAP1 Signaling Axis

Advanced Science, EarlyView.
This study reveals that Urolithin A (UA) counteracts alcohol‐induced cognitive and social dysfunction (AICSD) via a gut microbiome‐dependent mechanism. UA‐enriched Bacteroids sartorii and Parabacteroids distasonis elevate anandamide (AEA), which activates the CB1R‐DRD2‐Rap1 signaling cascade to drive synaptic repair and reduce neuroinflammation ...
Hongbo Zhang, Zibin Li, Yao Xiao, Ji Bian, Caian He, Chao Liu, Lan Gong, Lin Han, Zhigang Liu, Min Wang   +9 more
wiley   +1 more source

Evaluation of HIV-1 drug resistance in newly diagnosed individuals in Italy over the period 2017–2023

Journal of Global Antimicrobial Resistance
: Objective: We evaluated the prevalence of HIV-1 drug resistance in newly diagnosed individuals from 2017 to 2023, in Italy. Methods: Transmitted drug resistance (TDR) was evaluated by using the HIVdb algorithm (https://hivdb.stanford.edu/), through ...
A.C. Ka’e, F. Bassani, O. El Khalili, A. Bezenchek, F. Carli, A. Pupo, E. Gentilini Cacciola, L. Pezzati, L. Duca, I. Vicenti, W. Gennari, F. Lombardi, A. Shallvari, F. Saladini, V. Micheli, A. Cozzi-Lepri, A. Lai, M.M. Santoro, S. Rusconi   +18 more
doaj   +1 more source

HIV versus the Terminator: Drug resistance of HIV reverse transcriptase with mutations at the connection subdomain [PDF]

, 2008
only availableAntiretroviral drug therapy can prolong the life of an HIV-infected individual, but this treatment also promotes drug-resistance mutations.
Jackson, Jacob C., Sarafianos, Stefan G., Schuckmann, Matthew M.   +2 more
core  

The kinesin Eg5 inhibitor K858 induces apoptosis but also survivin-related chemoresistance in breast cancer cells [PDF]

, 2016
Inhibitors of kinesin spindle protein Eg5 are characterized by pronounced antitumor activity. Our group has recently synthesized and screened a library of 1,3,4-thiadiazoline analogues with the pharmacophoric structure of K858, an Eg5 inhibitor.
CARRADORI, Simone, DE IULIIS, FRANCESCA, giantulli, sabrina, GIUFFRIDA, Anna, MILANA, Bernardina, SALERNO, GERARDO, SCARPA, Susanna, SILVESTRI, Ida, Taglieri, Ludovica   +8 more
core   +1 more source

Tendon Organoids Enable Functional Tendon Rejuvenation Through ALKBH5‐Dependent RNA Demethylation

Advanced Science, EarlyView.
FT organoids reverse the aged phenotype of tendon cells, reinstating a fetal‐like state. This breakthrough establishes a potent cell source for tendon tissue engineering, effectively advancing regenerative medicine. ABSTRACT Adult tendon injuries pose a major clinical challenge due to limited self‐repair capacity, resulting in suboptimal regeneration ...
Tian Qin, Aini Pan, Zhuoning Miao, Yanyan Zhao, Xianan Mo, Heng Sun, Chunmei Fan, Junyu Guo, Bingbing Wu, Weiliang Shen, Qiangqiang Zheng, Jun Lu, Xi Jiang, Zi Yin, Xiao Chen   +14 more
wiley   +1 more source

Inhibitors of HIV-1 Reverse Transcriptase—Associated Ribonuclease H Activity

Biology, 2012
HIV-1 enzyme reverse transcriptase (RT) is a major target for antiviral drug development, with over half of current FDA-approved therapeutics against HIV infection targeting the DNA polymerase activity of this enzyme. HIV-1 RT is a multifunctional enzyme
Michael A. Parniak, Stefan G. Sarafianos, Rieko Ishima, Krystal LaBarge, Tatiana Ilina   +4 more
doaj   +1 more source