Results 181 to 190 of about 20,922 (255)

An AKR1C3-activated kinase inhibitor prodrug. [PDF]

RSC Chem Biol
Li Z, Martinez M, Byun WS, Thathireddy A, Qiu T, Wang Y, Katzengruber L, Chouldjian A, Lu W, Ji W, Che J, Zhang T, Hinshaw SM, Gray NS.   +13 more
europepmc   +1 more source

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

Discovery of a Colon-Targeted Prodrug As an <i>Escherichia coli</i> Biofilm Inhibitor for Treating Inflammatory Bowel Disease. [PDF]

ACS Med Chem Lett
Shimizu T, Tago K, Yokoyama M, Nakamura K, Tokieda-Tanoue S, Kita A, Miyazaki S.   +6 more
europepmc   +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

Reversing adenosine-mediated immunosuppression in triple-negative breast cancer by synergistic chemo-immunotherapy via stimuli-responsive nanomedicines. [PDF]

EBioMedicine
Cheng X, Cai H, Li X, Zhang Y, Li S, Li Y, Hu N, Lui S, Jing J, Gong Q, Luo K.   +10 more
europepmc   +1 more source

Diltiazem N‐oxide, a novel ischaemia‐activated prodrug, prevents ischaemia‐induced ventricular fibrillation without off‐target adverse effects

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Ventricular fibrillation (VF) in coronary heart disease accounts for up to 70% of sudden cardiac death. We examined whether diltiazem N‐oxide (DNO) has ischaemia‐selective antiarrhythmic activity. Experimental Approach Randomised and blinded experiments were performed in rat isolated hearts and in anaesthetised rats to ...
Louise M. Hesketh, Gabriel A. Watson, Francesca Mazzacuva, Zoe Hoare, Thomas R. Eykyn, Michael J. Curtis   +5 more
wiley   +1 more source

An <i>H</i>-Phosphonate-Mediated Synthesis of Nucleotide-Pyranose Glycoconjugates. [PDF]

Org Lett
Guillaume T, Huang N, Smith M, Miller GJ.   +3 more
europepmc   +1 more source

Delivery of nano‐formulated drugs to solid tumours is selectively increased by co‐application of the vascular disrupting agent CA4P

British Journal of Pharmacology, EarlyView.
Background and purpose Nano‐formulated chemotherapeutics prolong systemic availability of drugs and can reduce systemic toxicity, but their accumulation in solid tumours is often limited and unpredictable. Broadly applicable strategies to selectively enhance tumour delivery are lacking.
Annabel Kitowski, Constanze Heise, Stefanie Sperling, Jasmin Hotz, Danica Bajic, Marina Rubey, Kathrin Klar, Georg Höfner, Julien Vollaire, Veronique Josserand, Jean‐Luc Coll, Oliver Thorn‐Seshold, Petar Marinković, Julia Thorn‐Seshold   +13 more
wiley   +1 more source

A reduction-sensitive lipophilic dihydroartemisinin prodrug in a self-microemulsifying drug delivery system for treating breast cancer lung metastasis via intestinal lymphatic transport. [PDF]

Int J Pharm X
Zheng B, He C, Zhao F, Li R, Zhang Z, Chen X, Shi M, He B, Wang R, Ren G, Zhang S, Yang S.   +11 more
europepmc   +1 more source