Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

Translational advances in pancreatic ductal adenocarcinoma therapy

AN Hosein, SK Dougan, AJ Aguirre, A Maitra - Nature cancer, 2022 - nature.com
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer that is most frequently
detected at advanced stages, limiting treatment options to systemic chemotherapy with …

Therapeutic targeting of “undruggable” MYC

V Llombart, MR Mansour - EBioMedicine, 2022 - thelancet.com
Summary c-MYC controls global gene expression and regulates cell proliferation, cell
differentiation, cell cycle, metabolism and apoptosis. According to some estimates, MYC is …

[HTML][HTML] Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy

K Koikawa, S Kibe, F Suizu, N Sekino, N Kim, TD Manz… - Cell, 2021 - cell.com
Pancreatic ductal adenocarcinoma (PDAC) is characterized by notorious resistance to
current therapies attributed to inherent tumor heterogeneity and highly desmoplastic and …

Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

S Pan, A Ding, Y Li, Y Sun, Y Zhan, Z Ye… - Chemical Society …, 2023 - pubs.rsc.org
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

Clinical significance of FBXW7 loss of function in human cancers

J Fan, M Bellon, M Ju, L Zhao, M Wei, L Fu, C Nicot - Molecular cancer, 2022 - Springer
Abstract FBXW7 (F-Box and WD Repeat Domain Containing 7)(also referred to as FBW7 or
hCDC4) is a component of the Skp1-Cdc53/Cullin-F-box-protein complex (SCF/β-TrCP). As …

Advances in high‐throughput mass spectrometry in drug discovery

ME Dueñas, RE Peltier‐Heap, M Leveridge… - EMBO Molecular …, 2023 - embopress.org
High‐throughput (HT) screening drug discovery, during which thousands or millions of
compounds are screened, remains the key methodology for identifying active chemical …

Delineating cysteine-reactive compound modulation of cellular proteostasis processes

AR Julio, F Shikwana, C Truong, NR Burton… - Nature Chemical …, 2024 - nature.com
Covalent modulators and covalent degrader molecules have emerged as drug modalities
with tremendous therapeutic potential. Toward realizing this potential, mass spectrometry …

Reciprocal antagonism of PIN1-APC/CCDH1 governs mitotic protein stability and cell cycle entry

S Ke, F Dang, L Wang, JY Chen, MT Naik, W Li… - Nature …, 2024 - nature.com
Induced oncoproteins degradation provides an attractive anti-cancer modality. Activation of
anaphase-promoting complex (APC/CCDH1) prevents cell-cycle entry by targeting crucial …

Cis P-tau is a central circulating and placental etiologic driver and therapeutic target of preeclampsia

S Jash, S Banerjee, S Cheng, B Wang, C Qiu… - Nature …, 2023 - nature.com
Preeclampsia (PE) is the leading cause of maternal and fetal mortality globally and may
trigger dementia later in life in mothers and their offspring. However, the etiological drivers …