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Aug 21,2023
TAK-931ÊÇÒ»ÖÖ¸ßЧµÄCDC7ÒÖÖÆ¼Á£¬Í¨¹ýÒÖÖÆCDC7À´ÒÖÖÆDNA¸´ÖÆ£¬¾ßÓп¹Ö×Áö¹¦Ð§£¬ÌåÄÚҩЧÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell divis
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Jul 06,2023
IAPµ°°×ÊÇÓÐÎüÒýÁ¦µÄ°©Ö¢ÖÎÁưе㡣SM-406 ÊÇÒ»ÖÖ¿Ú·þÓÐЧµÄIAPÞ׿¹¼Á¡£SM-406 ÔÚÐÛÐÔSD´óÊ󡢱ȸñÈ®ºÍNHPÖеÄPKÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms.?The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators.
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Jul 06,2023
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Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric c
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Jul 06,2023
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Liver cancer is the fourth greatest cause of cancer related mortality. AD80 is a multi-kinase inhibitor with anti-tumoral activity across a variety of hepatocellular carcinoma (HCC) preclinical models
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Jul 06,2023
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Sulfonylureas exert their anti-diabetic effects by inhibiting K-ATP channels in the plasma membrane of islet ¦Â-cells. Chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to produce
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Jul 06,2023
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Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through
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Jul 05,2023
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Overexpression of VEGFR2 can offset the rescue effect of Apatinib on Paclitaxel-induced drug resistance of MGC803 cells. Apatinib inhibits Paclitaxel resistance of MGC803 cells via the VEGFR2 #signali
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Jul 05,2023
Ñо¿ÈËÔ±±¨¸æÁËÒ»ÖÖ¾ßÓÐϸ°ûÉøÍ¸ÐÔµÄÑ¡ÔñÐÔMETTL3ÄÉĦ¶ûÒÖÖÆ¼ÁUZH1a£¬×÷Õ߸ÐлÃÀµÏÎ÷ºÏ³ÉÁËUZH1aºÍUZH1b
The methylase METTL3 is the writer enzyme of the N6©\methyladenosine (m6A) modification of RNA.Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell©\permeable, whi
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Jul 05,2023
RIPK2¼¤Ã¸²ÎÓë¶àÖÖÂýÐÔÑ×Ö¢£¬UH15-15ÒÖÖÆRIPK2¼¤Ã¸²¢¾ßÓÐÁ¼ºÃµÄÌåÍâADMEºÍPKÌØÐÔ£¬PKÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
Receptor interacting protein kinase-2 (#RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous
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Jul 05,2023
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PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified com
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Jul 05,2023
zapERtrap£º¹âµ÷½ÚµÄÄÚÖÊÍøÊÍ·Åϵͳ½ÒʾÁËÒâÏë²»µ½µÄÉñ¾­ÔªÔËÊä;¾¶£¬ZapalogµÄºÏ³Éͨ¹ýÃÀµÏÎ÷½øÐÐ
zapERtrap opens the door to previously unapproachable questions concerning how proteins are processed, trafficked, and secreted in space and time in complex cellular environments. zapERtrap relies on
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Jul 05,2023
Ñо¿ÈËԱʹÓÃRZ-2994À´±íÕ÷ÒÖÖÆSHMT1/2ÔÚTϸ°û¼±ÐÔÁܰÍϸ°û°×Ѫ²¡ (T-ALL) ÖеÄ×÷Óã¬RZ-2994ͨ¹ýÃÀµÏÎ÷¶¨ÖƺϳÉ
Despite progress in the treatment of T-cell acute lymphoblastic leukemia (T-ALL) has limited treatment options, particularly in the setting of relapsed/refractory disease. Researchers used SHMT1/2 inh
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Jul 05,2023
Ñо¿ÈËÔ±¿ª·¢ÁËÒ»ÖÖ¸ßÌØÒìÐÔµÄCDC7ÒÖÖÆ¼ÁTAK-931×÷ΪÁÙ´²Ö×ÁöÖÎÁƼÁ£¬¿¹Ö×ÁöҩЧÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
Cell division cycle 7 (CDC7) plays important roles in DNA replication. Researchers developed a highly specific CDC7 inhibitor, TAK-931, as a clinical cancer therapeutic agent. The antitumor efficacy s
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Ñо¿ÈËÔ±¿ª·¢ÁËÒ»ÖÖ¸ßÌØÒìÐÔµÄCDC7ÒÖÖÆ¼ÁTAK-931×÷ΪÁÙ´²Ö×ÁöÖÎÁƼÁ£¬¿¹Ö×ÁöҩЧÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
Jul 05,2023
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RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers r
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Jun 28,2023
ARD-2128ÊÇÒ»ÖÖPROTAC AR½µ½â¼Á£¬¾ßÓгöÉ«µÄѪ½¬ºÍ΢Á£ÌåÎȶ¨ÐÔ£¬ÌåÍâÎȶ¨ÐÔºÍPKÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.
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ARD-2128ÊÇÒ»ÖÖPROTAC AR½µ½â¼Á£¬¾ßÓгöÉ«µÄѪ½¬ºÍ΢Á£ÌåÎȶ¨ÐÔ£¬ÌåÍâÎȶ¨ÐÔºÍPKÑо¿Í¨¹ýÃÀµÏÎ÷½øÐÐ
Jun 28,2023
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Radiation therapy is used as the primary treatment for lung cancer. In this study, radiation therapy for establish ionizing radiation-resistant lung cancer cell lines (A549-IR/H1299-IR) was supported by Medicilon.
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Jun 28,2023
CAR-TÁÆ·¨Ö÷ÒªÕë¶Ô°×Ѫ²¡Óë¶ñÐÔÁܰÍÁö£¬´ËÑо¿Öй¹½¨³ÁĬPD-1µÄshRNAÔØÌåÖÊÁ££¬²âÐòºóÖÊÁ£µÄ¼ø¶¨Í¨¹ýÃÀµÏÎ÷½øÐÐ
Chimeric antigen receptor T cells (CAR-T) immunotherapy has shown promising clinical results in the treatment of leukemia and lymphoma, but the effectiveness is limited for solid tumors. The shRNA vector plasmid that silences PD-1 and preparation of CAR i
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CAR-TÁÆ·¨Ö÷ÒªÕë¶Ô°×Ѫ²¡Óë¶ñÐÔÁܰÍÁö£¬´ËÑо¿Öй¹½¨³ÁĬPD-1µÄshRNAÔØÌåÖÊÁ££¬²âÐòºóÖÊÁ£µÄ¼ø¶¨Í¨¹ýÃÀµÏÎ÷½øÐÐ
Jun 28,2023
GS-5801ÊÇÒ»ÖÖÓÐЧµÄKDM5ÒÖÖÆ¼Á£¬¾ßÓп¹HBV»îÐÔ£¬GS-5801ͨ¹ýÃÀµÏÎ÷ºÏ³É
GS-5801, a potent inhibitor of KDM5, has antiviral activity against HBV in a primary human hepatocytes infection model, with the cellular permeability, oral bioavailability. GS-5801 was synthesized by Medicilon.
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GS-5801ÊÇÒ»ÖÖÓÐЧµÄKDM5ÒÖÖÆ¼Á£¬¾ßÓп¹HBV»îÐÔ£¬GS-5801ͨ¹ýÃÀµÏÎ÷ºÏ³É
Jun 28,2023
TR-107ÊÇÈËÀàÏßÁ£Ìåµ°°×øClpPµÄÓÐЧ¼¤»î¼Á£¬PK·ÖÎöͨ¹ýÃÀµÏÎ÷½øÐÐ
The pharmacokinetic properties of TR©\107 were compared with other known ClpP activators including ONC201 and ONC212. TR©\107 displayed excellent exposure and serum t1/2 after oral administration. Pharmacokinetic analysis were evaluated for pharmacokinetic
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TR-107ÊÇÈËÀàÏßÁ£Ìåµ°°×øClpPµÄÓÐЧ¼¤»î¼Á£¬PK·ÖÎöͨ¹ýÃÀµÏÎ÷½øÐÐ
Jun 16,2022
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