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 …
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …
Translational advances in pancreatic ductal adenocarcinoma therapy
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer that is most frequently
detected at advanced stages, limiting treatment options to systemic chemotherapy with …
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 …
differentiation, cell cycle, metabolism and apoptosis. According to some estimates, MYC is …
[HTML][HTML] Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy
Pancreatic ductal adenocarcinoma (PDAC) is characterized by notorious resistance to
current therapies attributed to inherent tumor heterogeneity and highly desmoplastic and …
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
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 …
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 …
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 …
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 …
with tremendous therapeutic potential. Toward realizing this potential, mass spectrometry …
Reciprocal antagonism of PIN1-APC/CCDH1 governs mitotic protein stability and cell cycle entry
Induced oncoproteins degradation provides an attractive anti-cancer modality. Activation of
anaphase-promoting complex (APC/CCDH1) prevents cell-cycle entry by targeting crucial …
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
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 …
trigger dementia later in life in mothers and their offspring. However, the etiological drivers …