Mer tyrosine kinase (MerTK) is aberrantly elevated in various tumor cells and has a normal anti-inflammatory role in the innate immune system. Inhibition of MerTK may provide dual effects against these MerTK-expressing tumors through reducing cancer cell survival and redirecting the innate immune response. Recently, we have designed novel and potent macrocyclic pyrrolopyrimidines as MerTK inhibitors using a structure-based approach. The most active macrocycles had an EC<sub>50</sub> below 40 nM in a cell-based MerTK phosphor-protein ELISA assay. The X-ray structure of macrocyclic analogue <b>3</b> complexed with MerTK was also resolved and demonstrated macrocycles binding in the ATP binding pocket of the MerTK protein as anticipated. In add...
We report herein the design, synthesis, and evaluation of macrocyclic peptidomimetics that bind to W...
This thesis describes the development of two anticancer drug leads from macrocyclic peptide-based ...
Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles ...
Mer tyrosine kinase (MerTK) is aberrantly elevated in various tumor cells and has a normal anti-infl...
Macrocycles have attracted significant attention in drug discovery recently. In fact, a few de novo ...
With over 500 family members, kinases are key mediators of many important disease relevant signaling...
ABSTRACT: The role of Mer kinase in regulating the second phase of platelet activation generates an ...
Macrophages are important cellular effectors in innate immune responses and play a major role in aut...
Mycobacterium tuberculosis thymidylate kinase (MtTMPK) has emerged as an attractive target for ratio...
Abnormal activation or overexpression of Mer receptor tyrosine kinase has been implicated in surviva...
Ectopic Mer expression promotes pro-survival signaling and contributes to leukemogenesis and chemore...
ABSTRACT: We previously reported a potent small molecule Mer tyrosine kinase inhibitor UNC1062. Howe...
The TAM (Axl, Mer, and Tyro3) family is implicated in the survival and chemoresistance of tumours an...
Microtubule associated serine/threonine kinase (MASTL) is an important Ser/Thr kinase belonging to ...
Although all kinases share the same ATP binding pocket, subtle differences in the residues that form...
We report herein the design, synthesis, and evaluation of macrocyclic peptidomimetics that bind to W...
This thesis describes the development of two anticancer drug leads from macrocyclic peptide-based ...
Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles ...
Mer tyrosine kinase (MerTK) is aberrantly elevated in various tumor cells and has a normal anti-infl...
Macrocycles have attracted significant attention in drug discovery recently. In fact, a few de novo ...
With over 500 family members, kinases are key mediators of many important disease relevant signaling...
ABSTRACT: The role of Mer kinase in regulating the second phase of platelet activation generates an ...
Macrophages are important cellular effectors in innate immune responses and play a major role in aut...
Mycobacterium tuberculosis thymidylate kinase (MtTMPK) has emerged as an attractive target for ratio...
Abnormal activation or overexpression of Mer receptor tyrosine kinase has been implicated in surviva...
Ectopic Mer expression promotes pro-survival signaling and contributes to leukemogenesis and chemore...
ABSTRACT: We previously reported a potent small molecule Mer tyrosine kinase inhibitor UNC1062. Howe...
The TAM (Axl, Mer, and Tyro3) family is implicated in the survival and chemoresistance of tumours an...
Microtubule associated serine/threonine kinase (MASTL) is an important Ser/Thr kinase belonging to ...
Although all kinases share the same ATP binding pocket, subtle differences in the residues that form...
We report herein the design, synthesis, and evaluation of macrocyclic peptidomimetics that bind to W...
This thesis describes the development of two anticancer drug leads from macrocyclic peptide-based ...
Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles ...