Knowledge Library
Evaluation of Bispecific Antibodies in NHPs
In recent years, bispecific antibodies (BsAbs) have emerged as a novel strategy in tumor immunotherapy. BsAbs combine two distinct antigen targets within a single antibody molecule, potentially enhancing clinical efficacy and safety. As a result of this dual targeting approach, the clinical therapeutic effects of BsAbs are considered superior to those of monoclonal antibodies. WuXi …Read More >
Highly Selective Novel Heme Oxygenase-1 Hits Found by DNA-Encoded Library ML
The heme oxygenase (HO) family comprises the major isozymes HO-1 and HO-2, of which HO-1 is deemed as an emerging target for cancer therapy. HO-1 overexpression is often observed in prostate, renal, colon, lung, breast, and glioma cancers. In a publication in ACS Med Chem Letters, WuXi AppTec scientists report the discovery of five series …Read More >
Empowering Early Discovery of Peptide Drugs
In this webinar, our experts discuss recent advancements in peptide drug discovery, including the evolution of mRNA display and peptide DNA-encoded library (DEL) technology for hit generation and selection, as well as novel cyclization techniques and their combinations for peptide conformational rigidity. This webinar offers a comprehensive perspective on strategies that are crucial for achieving …Read More >
Discovery of Potent, Selective, and Orally Available IRE1 alpha Inhibitors
Inositol-requiring enzyme 1α (IRE1α) is a sensor protein that plays a key role in multiple myeloma (MM) and is a potential therapeutic target for this type of blood cancer. IRE1α is activated by ER stress, which is common in MM cells due to their high protein synthesis. WuXi AppTec recently contributed to a study which …Read More >
Discovery of SARS-CoV-2 Papain-like Protease Inhibitors
SARS-CoV-2 antivirals which have been clinically approved or are in late-stage development are directed against either the RNA-dependent RNA polymerase (RdRp) or the main protease (Mpro). With the possibility of resistance developing over time, there is a need for additional oral antivirals directed against currently undrugged viral targets. Conserved across coronaviruses, the SARS-CoV-2 papain-like protease …Read More >
Research Strategies for the Discovery of Targeted Protein Degraders
In this webinar, experts present research strategies for the discovery of targeted protein degraders. Over the past decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. Since 2016, WuXi AppTec has built a comprehensive TPD discovery service platform, adept in over 20 …Read More >
Pharmacodynamic and Pharmacokinetic Profile of a Novel GLP-1 Receptor Biased Agonist
Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However, because of the continued need for injectable administration, many GLP-1 agonists face compliance challenges. To improve the design and production of GLP-1 receptor biased agonists with enhanced druggability, a novel small molecule, designated SAL0112, was …Read More >
USP7 Inhibitors Reveal a Differentiated Mechanism of p53-Driven Anti-Cancer Activity
Ubiquitin-specific protease 7 (USP7) is a deubiquitinating enzyme that cleaves ubiquitin from a range of substrates, shielding them from degradation by the proteasome. USP7 activity has been implicated in cancer progression and its overexpression is associated with tumor aggressiveness and poor prognosis in a variety of cancer types, making USP7 inhibition an attractive strategy for …Read More >
A µ-Opioid Receptor Modulator that Works Cooperatively with Naloxone
G-protein coupled receptors (GPCRs) play a pivotal role in signaling pathways, and these transmembrane proteins represent an important drug target class. The majority of approved drugs that target GPCRs bind to traditional orthosteric sites. In a recent publication in Nature, Professor Brian Kobilka and his team at Stanford University successfully identified selective negative allosteric modulators …Read More >