Results 71 to 80 of about 33,063 (219)

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

AKTIVITAS ANTIOKSIDAN EKSTRAK BUNGA WIJAYA KUSUMA (Epiphyllum oxypetalum)

Jurnal Ilmiah Medicamento, 2018
Telah dilakukan isolasi dan uji screening fitokimia fraksi antioksidan dari bunga wijaya kusuma (Epiphyllum oxypetalum). Ekstraksi metabolitnya dilakukan secara maserasi menggunakan metanol sehingga dihasilkan 45,2579 gram ekstrak kental metanol ...
Ni Putu Rahayu Artini, I Wayan Tanjung Aryasa   +1 more
doaj  

In-depth LC-MS and in-vitro studies of a triterpenoid saponin capilliposide-A metabolism modulation in gut microbiota of mice

Frontiers in Pharmacology
Introduction: Some herbal ingredients can reshape the composition of the gut microbiome as well as its metabolites. At the same time, the gut microbiota can also affect drug metabolism.
Huan Zhao, Huan Zhao, Xueli Hu, Shenghong Guan, Jinhong Cai, Xiaohan Li, Jiaxi Fang, Bo Lin, Wei Zhu, Jingkui Tian, Juan Jin, Qiang He, Qiang He, Xiaoyong Zhang   +13 more
doaj   +1 more source

Therapeutic potential of natural products in cancer immunotherapy: Advances and challenges

British Journal of Pharmacology, EarlyView.
This review systematically outlines the mechanisms underlying tumour immunotherapy resistance and elucidates the role of natural products in enhancing therapeutic efficacy as immunomodulatory adjuvants. Abstract Immunotherapy has emerged as a clinically pivotal approach in cancer treatment, but its application remains limited to a small subset of ...
Rao Hu, Kaibin Dai, Zhensheng Lin, Mingfang Ye, Minfeng Chen, Xiaobo Li, Dongmei Zhang   +6 more
wiley   +1 more source

The Triterpenoid CDDO-Methyl Ester Reduces Tumor Burden, Reprograms the Immune Microenvironment, and Protects from Chemotherapy-Induced Toxicity in a Preclinical Mouse Model of Established Lung Cancer

Antioxidants
NRF2 activation protects epithelial cells from malignancy, but cancer cells can upregulate the pathway to promote survival. NRF2 activators including CDDO-Methyl ester (CDDO-Me) inhibit cancer in preclinical models, suggesting NRF2 activation in other ...
Jessica A. Moerland, Karen T. Liby
doaj   +1 more source

Thermodynamic characterisation of covalent ligand binding

British Journal of Pharmacology, EarlyView.
Background and Purpose Differential scanning fluorimetry (DSF) is a common and straightforward method to evaluate the thermal stability of proteins and has been heavily used for ligand binding characterisation as well as for screening. One class of compounds that is less typically evaluated by DSF are covalent binders.
Rebecca Hertzman, Maayan Lavie, Almog Nadir, Ronen Gabizon, Nir London   +4 more
wiley   +1 more source

Distributions of Lanostene-Derived Triterpenoids and Glucan Content in the Fruiting Bodies of the Australian Ganoderma Species

Journal of Fungi
Lanostene-derived triterpenoids and β-glucans are important metabolites in Ganoderma mushrooms associated with benefits to human health. The medicinal value of the Australian Ganoderma species remains unclear, with no data on triterpenoid distribution or
Aline De Oliveira Campos, Mark D. Harrison, David L. Marshall, Peter James Strong   +3 more
doaj   +1 more source

CD36‐mediated lipid rewiring in the metabolic adaptation of tumour ecosystems

The FEBS Journal, EarlyView.
Nutrient deprivation drives a lipid‐centric shift in tumour metabolic symbiosis and signalling network. CD36 functions as a bidirectional bridge, transferring fatty acids from stromal donors (adipocytes, CAFs) to the ecosystem tumour‐ and microenvironment‐dependently.
Anna Sebestyén, Viktória Varga, Fatime Szalai, Risa Miyaura, Nóra Förhécz, Bálint Csikós, Rebeka Gelencsér, Zsófia Gábriel, Timea Komlódi, Katalin Dezső, Ildikó Krencz, Dorottya Moldvai   +11 more
wiley   +1 more source

Directional information flow in human frataxin defines allosteric pathways connecting the hydrophobic core to the iron‐binding ridge

The FEBS Journal, EarlyView.
Human frataxin deficiency causes Friedreich's ataxia, yet how iron‐binding events are communicated across the protein is unclear. Using transfer entropy analysis of molecular dynamics simulations, we identify buried hydrophobic core leucines (LEU136, LEU140) as the source of directional signaling toward the iron‐binding acidic ridge.
Kevser Kübra Kırboğa, Ecir Uğur Küçüksille   +1 more
wiley   +1 more source

Synergistic enhancement SPF from annatto seed oil and alkaline extracts in association with organic UV filters

International Journal of Cosmetic Science, EarlyView.
An SPF formulation incorporating Bixa orellana seed extracts and oils showed enhanced UV protection, highlighting the potential of natural bioactive compounds as effective boosters in photoprotective cosmetic products. Abstract Objective This study investigated the antioxidant activity of oil and alkaline aqueous extracts obtained from Bixa orellana ...
Ister Cordeiro Mariotini, Aliny Rodrigues de Jesus da Conceição, Rodrigo Rezende Kitagawa, Bernardo de Jesus Pavuna, Claudia Masrouah Jamal, Claudineia Aparecida Sales de Oliveira Pinto, André Rolim Baby, Fabiana Vieira Lima Solino Pessoa, Mariana Santos Pinheiro   +8 more
wiley   +1 more source