Results 121 to 130 of about 287,149 (254)

A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova, Thomas M. Geiger, Lorenzo Cianni, Dominika E. Pieńkowska, Jan Gerhartz, Lina Read, Aleša Bricelj, Alexander Herrmann, Maurice Leon Nelles, Yuen Lam Dora Ng, Marcus D. Hartmann, Jan Krönke, Izidor Sosič, Radosław P. Nowak, Michael Gütschow, Christian Steinebach   +15 more
wiley   +1 more source

When Cofactors Aren't X Factors: Functional Groups That Are Labile in Human Liver Microsomes in the Absence of NADPH. [PDF]

ACS Med Chem Lett, 2022
Landry ML, Trager R, Broccatelli F, Crawford JJ.   +3 more
europepmc   +1 more source

4‐(5‐Chloro‐3‐(3,4,5‐trimethoxybenzoyl)‐1H‐indol‐1‐yl)benzenesulfonamide: A Novel Polypharmacology Agent to Target Carbonic Anhydrase IX and XII With Improved Selectivity, Wnt/β‐Catenin Signaling Pathway, and P‐Glycoprotein

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
Polypharmacology is expected to produce higher therapeutic efficacy and lower cytotoxic and side effects. Compound 15 exhibited strong inhibition of the human carbonic anhydrase isoforms IX and XII and selectivity toward the adverse isoforms I and II.
Michela Puxeddu, Rosa Bordone, Claudia Colla, Gabriele Rotili, Antonio Coluccia, Pietro Sciò, Petra Cuřínová, Alessio Nocentini, Claudiu T. Supuran, Serena Filiberti, Marta Turati, Roberto Ronca, Joanna Kopecka, Chiara Riganti, Lucia Jimenez, Wolfgang Link, Chiara Bigogno, Giulio Dondio, Martina Barba, Gianluca Canettieri, Romano Silvestri, Giuseppe La Regina   +21 more
wiley   +1 more source

Herb-drug interaction of Astragali Radix based on in vitro incubation and pharmacokinetic assessment

BMC Complementary Medicine and Therapies
Background Astragali Radix (AR) is extensively utilized in Asia for its various pharmacological effects. With the widespread use of AR, the risk of herb-drug interactions (HDIs) mediated by cytochrome P450 (P450) enzymes has become a serious concern ...
Tianwang Wang, Tingting Zhang, Xiaofei Chen, Chonggang Huang, Pengfei Tu, Kai Wang, Feng Qiu   +6 more
doaj   +1 more source

Similar 5F-APINACA Metabolism between CD-1 Mouse and Human Liver Microsomes Involves Different P450 Cytochromes. [PDF]

Metabolites, 2022
Crosby SV, Ahmed IY, Osborn LR, Wang Z, Schleiff MA, Fantegrossi WE, Nagar S, Prather PL, Boysen G, Miller GP.   +9 more
europepmc   +1 more source

An Imidazo[2,1‐b][1,3,4]thiadiazole Derivative Inhibits the Virulence Factor α‐Hemolysin by Blocking the Pullout of Its Stem Domain

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
A high‐throughput cellular screen based on Ca2+ influx in U937 monocytic cells identified thiadiazoles as small‐molecule inhibitors of α‐hemolysin, a key virulence factor of Staphylococcus aureus. The thiadiazole 1 prevents pore formation by a dual mechanism that prevents stem loop unfolding as well as membrane attachment.
Vadim S. Korotkov, Peer Lukat, Raffaella Di Lucrezia, Aditya Shekhar, Carsten Degenhart, Randi Diestel, Ursula Bilitewski, Klaus Dinkel, Wulf Blankenfeldt, Mark Brönstrup   +9 more
wiley   +1 more source

Metabolism of Diterpenoids Derived from the Bark of Cinnamomum cassia in Human Liver Microsomes. [PDF]

Pharmaceutics, 2021
Choi SM, Pham VC, Lee S, Kim JA.
europepmc   +1 more source

Oxidative metabolism of BDE-99 by human liver microsomes: predominant role of CYP2B6.

Toxicological Sciences, 2012
C. Erratico, A. Szeitz, S. Bandiera
semanticscholar   +1 more source

A validated LC-MS/MS analytical method for the quantification of pemigatinib: metabolic stability evaluation in human liver microsomes. [PDF]

RSC Adv, 2022
Attwa MW, Abdelhameed AS, Alsaif NA, Kadi AA, AlRabiah H.   +4 more
europepmc   +1 more source

Exploring the Interactome of Cytochrome P450 2E1 in Human Liver Microsomes with Chemical Crosslinking Mass Spectrometry. [PDF]

Biomolecules, 2022
Davydov DR, Dangi B, Yue G, Ahire DS, Prasad B, Zgoda VG.   +5 more
europepmc   +1 more source