TY 101 / Tayu Huaxia Biotech - LARVOL DELTA

3D-QSAR, molecular docking, molecular dynamics, and ADME/T analysis of marketed and newly designed flavonoids as inhibitors of Bcl-2 family proteins for targeting U-87 glioblastoma. (PubMed, J Cell Biochem) - "The molecular docking study revealed that BCL-XL has a higher binding affinity with the most active compounds, and the MD simulation showed that some residues of the BH3 domain, such as Phe97, Tyr101, Arg102, and Phe105 create remarkable hydrophobic interactions with the ligands. 3D-QSAR study is a beneficial method to evaluate and design anticancer compounds. Considering the results of the molecular docking study, MD simulation, and ADME/T analysis, the designed compound 54 could be considered as a potential treatment for glioblastoma."

Journal • Brain Cancer • Glioblastoma • Oncology • Solid Tumor • BCL2 • BCL2L1

A TNFR2 antibody by countering immunosuppression cooperates with HMGN1 and R848 immune stimulants to inhibit murine colon cancer. (PubMed, Int Immunopharmacol) - "The result also suggested that the effect of TY101 was similar to that of anti-PD-L1 when used in combination with these immunostimulants. Therefore, we propose that treatment strategies of antagonizing TNFR2 on Tregs would behave as potent checkpoint inhibitors and can potentially be utilized to develop a novel antitumor immunotherapy."

Journal • Preclinical • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • CD8 • TLR4 • TNFRSF1B

A Phase 1/2 Study of TY101 for Locally Advanced /Metastatic Solid Tumors and Relapsed or Refractory Lymphomas (clinicaltrials.gov) - P1/2; N=268; Recruiting; Sponsor: Tayu Huaxia Biotech Medical Group Co., Ltd.; Not yet recruiting ➔ Recruiting; Initiation date: Aug 2020 ➔ Dec 2020

Clinical • Enrollment open • Trial initiation date • Gastrointestinal Cancer • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • PD-L1

The Dual-Targeting Activity of the Metabolite Substrate of Para-amino Salicyclic Acid in the Mycobacterial Folate Pathway: Atomistic and Structural Perspectives. (PubMed, Protein J) - "Similarly, the binding of PAS-M towards FDTS also involved consistent strong conventional hydrogen bond interactions between some specific residues (Tyr101, Arg172, Thr4, Gln103, Arg87 and Gln106) and, the 2-amino-decahydropteridin-4-ol group, thus establishing the cruciality of the group. These conformational changes possibly interfered with the biological functions of the enzymes and hence their inhibition as experimentally reported. Structural Insights provided could open up a novel paradigm of structure-based design of multi-targeting inhibitors of biological targets in the folate biosynthetic pathway toward tuberculosis therapy."

Journal • Infectious Disease • Respiratory Diseases • Tuberculosis

[VIRTUAL] A pan-cancer study of GNAQ/GNA11 mutations in Chinese cancer patients (ESMO 2020) - "The most common mutations of protein change was p.Thr96Ser (20.5%), followed by p.Tyr101* (14.5%) and p.Lys322Asn (2.6%), which mainly occurred in exon 2 (2/7) and exon7 (7/7)...Legal entity responsible for the study: Inner Mongolia People's Hospital. Funding: Has not received any funding."

Clinical • Pan Tumor • Biliary Cancer • Cholangiocarcinoma • Gastric Cancer • Gastrointestinal Cancer • Glioma • Melanoma • Oncology • Solid Tumor • Uveal Melanoma • CREBBP • GNA11 • GNAQ • KMT2D • LRP1B • MLL3 • TP53

A Phase 1/2 Study of TY101 for Locally Advanced /Metastatic Solid Tumors and Relapsed or Refractory Lymphomas (clinicaltrials.gov) - P1/2; N=268; Not yet recruiting; Sponsor: Tayu Huaxia Biotech Medical Group Co., Ltd.

Clinical • New P1/2 trial • Gastrointestinal Cancer • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor