Molchanova, Natalia Wang, Hengzhuang Hansen, Paul R. Høiby, Niels Nielsen, Hanne M. Franzyk, Henrik
Published in
Frontiers in Microbiology
Pseudomonas aeruginosa infection is a predominant cause of morbidity and mortality in patients with cystic fibrosis infection and with a compromised immune system. Emergence of bacterial resistance renders existing antibiotics inefficient, and therefore discovery of new antimicrobial agents is highly warranted. In recent years, numerous studies hav...
Liu, Bee Hui Jobichen, Chacko Chia, C S Brian Chan, Tim Hon Man Tang, Jing Ping Chung, Theodora X Y Li, Jia Poulsen, Anders Hung, Alvin W Koh-Stenta, Xiaoying
...
Published in
Proceedings of the National Academy of Sciences of the United States of America
Sal-like 4 (SALL4) is a nuclear factor central to the maintenance of stem cell pluripotency and is a key component in hepatocellular carcinoma, a malignancy with no effective treatment. In cancer cells, SALL4 associates with nucleosome remodeling deacetylase (NuRD) to silence tumor-suppressor genes, such as PTEN. Here, we determined the crystal str...
Knight, J Morgan Mandal, Pijus Morlacchi, Pietro Mak, Garbo Li, Evan Madison, Matthew Landers, Cameron Saxton, Brandon Felix, Ed Gilbert, Brian
...
Published in
The Journal of biological chemistry
Asthma is a chronic inflammatory disease of the lungs and airways and one of the most burdensome of all chronic maladies. Previous studies have established that expression of experimental and human asthma requires the IL-4/IL-13/IL-4 receptor α (IL-4Rα) signaling pathway, which activates the transcription factor STAT6. However, no small molecules t...
Gong, Caifeng Valduga, Julie Chateau, Alicia Richard, Mylène Pellegrini-Moïse, Nadia Barberi-Heyob, Muriel Chastagner, Pascal Boura, Cédric
Published in
Oncotarget
Medulloblastoma (MB) is the most common malignant pediatric brain tumor. Despite the progress of new treatments, the risk of recurrence, morbidity, and death remains important. The neuropilin-1 (NRP-1) receptor has recently been implicated in tumor progression of MB, which seems to play an important role in the phenotype of cancer stem cells. Targe...
Pallerla, Sandeep Naik, Himgauri Singh, Sitanshu Gauthier, Ted Sable, Rushikesh Jois, Seetharama D.
Published in
Journal of peptide science : an official publication of the European Peptide Society
HER2 receptors are surface proteins belonging to the epidermal growth factor family of receptors (EGFR). Their numbers are elevated in breast, lung, and ovarian cancers. HER2-positive cancers are aggressive, higher mortality rate and have a poor prognosis. We have designed peptidomimetics that bind to HER2 and block the HER2-mediated dimerization o...
Tala, Srinivasa R. Singh, Anamika Lensing, Cody J. Schnell, Sathya M. Freeman, Katie T. Rocca, James R. Haskell-Luevano, Carrie
Published in
ACS chemical neuroscience
Kokel, Anne Torok, Marianna
Published in
Current medicinal chemistry
Since the first isolation of antimicrobial peptides (AMPs) they have attracted extensive interest in medicinal chemistry. However, only a few AMP-based drugs are currently available on the market. Despite their effectiveness, biodegradability, and versatile mode of action that is less likely to induce resistance compared to conventional antibiotics...
Kobayakawa, Takuya Matsuzaki, Yudai Hozumi, Kentaro Nomura, Wataru Nomizu, Motoyoshi Tamamura, Hirokazu
Published in
ACS Medicinal Chemistry Letters
The first rapid and efficient chemical synthesis of a cyclic Arg-Gly-Asp (RGD) peptide containing a chloroalkene dipeptide isostere (CADI) is reported. By a developed synthetic method, an N - tert -butylsulfonyl protected CADI was obtained utilizing diastereoselective allylic alkylation as a key reaction. This CADI was also transformed into an N -F...
Sverchinsky, Dmitry V Lazarev, Vladimir F Semenyuk, Pavel I Mitkevich, Vladimir A Guzhova, Irina V Margulis, Boris A
Published in
FEBS letters
Most Hsp70 chaperone inhibitors exert anti-cancer effects; however, their high cytotoxicity proposed the use of peptide fragments of the chaperone as safer modulators of its activity and as complements to customary drugs. One such peptide, ICit-2, was found to inhibit substrate-binding and refolding activities of the chaperone. Using various approa...
Thakkar, Balmukund Sureshkumar Albrigtsen, Marte Svendsen, John Sigurd Andersen, Jeanette H Engh, Richard Alan
Published in
Chemical biology & drug design
Drug discovery strategies include from broad random screening to focussed target-based approaches. Structure and substrate information greatly enables target-based design, but this is limited to relatively few targets; cell-based screening can identify new targets but often suffers from low hit rates and difficult hit optimization. Thus, newer appr...
