Results 161 to 170 of about 823,777 (226)

Hijacking the MDM2 E3 Ligase with Novel BRD4‐Targeting Proteolysis‐Targeting Chimeras in Pancreatic Cancer Cells

The phenotypic effect induced by a Proteolysis‐Targeting Chimera (PROTAC) can depend on several factors, including the E3 ligase recruited. For the discovery of a first‐in‐class PROTAC for a target of interest, the E3 ligases commonly hijacked remain the
Springer, C. J., Aljarah, M., Niculescu‐Duvaz, Dan, Aljarah, Mohammed, Niculescu-Duvaz, Dan, Ficu, Mihaela P., Springer, Caroline J., Ficu, M. P., Kershaw, Christopher S., Niculescu-Duvaz, D., Kershaw, C. S.   +10 more
core   +1 more source

Dual FLT3/MAPK14 Proteolysis-Targeting Chimera (PROTAC) Induces Potent Acute Myeloid Leukemia Cell Death. [PDF]

Pharmaceuticals (Basel)
Abdelsalam M, Halilovic M, Ashry R, Nassar H, Erdmann F, Schmidt M, Krämer OH, Sippl W.   +7 more
europepmc   +1 more source

Proteolysis Targeting Chimera (PROTAC) Linkerology Enhances the CDK-Degradation Selectivity Profile of a Multi-CDK Inhibitor: Discovery of Potent, Anti-Leukemic CDK9 Degraders. [PDF]

ACS Pharmacol Transl Sci
Chan AM, Eberly C, Goodis CC, Nordquist EB, Weldemariam M, Carter-Cooper BA, Pogash S, Lapidus R, Kane MA, MacKerell AD, Civin CI, Fletcher S.   +11 more
europepmc   +1 more source

PROteolysis TArgeting Chimera (PROTAC) Estrogen Receptor Degraders for Treatment of Estrogen Receptor-Positive Advanced Breast Cancer. [PDF]

Target Oncol
Hamilton EP, Jeselsohn RM, Vahdat LT, Hurvitz SA.   +3 more
europepmc   +1 more source

Benchmark of protocols for the prediction of ternary complexes target–PROTAC–ligase, with potential application to the kinase CK1δ.

openLa presente tesi esplora l’impiego di tecniche di modellistica molecolare nello studio di PROTAC (PROteolysis TArgeting Chimera), una nuova classe di molecole terapeutiche in grado di indurre la degradazione selettiva di proteine bersaglio ...
JABBOUR, ROGER
core  

Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation. [PDF]

J Med Chem
Deng Z, Catlett J, Lee Y, Wu Q, Xu Z, Xie L, Chen X, Xiong Y, Kaniskan HÜ, Jin J.   +9 more
europepmc   +1 more source

Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole-nicotinamide chemotype. [PDF]

RSC Med Chem
Weldert AC, Frey AF, Krone MW, Krähe F, Kuhn H, Kersten C, Barthels F.   +6 more
europepmc   +1 more source

Discovery of a peptide proteolysis-targeting chimera (PROTAC) drug of p300 for prostate cancer therapy. [PDF]

EBioMedicine
Zhang D, Ma B, Liu D, Wu W, Zhou T, Gao Y, Yang C, Jian Y, Fan Y, Qian Y, Ma J, Gao Y, Chen Y, Xu S, Li L.   +14 more
europepmc   +1 more source

BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells. [PDF]

Leukemia, 2018
Sun B, Fiskus W, Qian Y, Rajapakshe K, Raina K, Coleman KG, Crew AP, Shen A, Saenz DT, Mill CP, Nowak AJ, Jain N, Zhang L, Wang M, Khoury JD, Coarfa C, Crews CM, Bhalla KN.   +17 more
europepmc   +1 more source

Correction to "Proteolysis-targeting chimera (PROTAC): current applications and future directions". [PDF]

MedComm (2020)
europepmc   +1 more source