I had an incredible time at #ACSSpring2025! The conference was filled with groundbreaking research and cutting-edge advancements in chemistry and biology, and I was truly amazed by the depth of innovation on display.
Anh-Tuan Pham
@astatinepham
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Instructor at BIDMC, Harvard Medical School
I had an incredible time at the AAAS Annual Meeting 2025 in Boston! This was my first experience at a multidisciplinary conference, and I gained valuable insights from areas outside my own field.
I’m so grateful to be a part of the AAAS community! #AAASmtg
I'm excited to share our work on the discovery of novel selective Orai blockers.
https://www.sciencedirect.com/science/article/abs/pii/S022352342400686X?via%3Dihub
The Orai channel is one of the major components of the calcium release activated calcium (CRAC) channel. The CRAC channel is highly expressed in T lymphocytes and plays critical role in regulating T cell proliferation and functions.
In this work, we describe structure-activity relationships of a series of selective Orai channel blockers.
Receptor-interacting serine/threonine kinase 2 (RIPK2) is a dual-specific kinase downstream of NODs signaling pathway. RIPK2 plays important roles in both innate and adaptive immunities. This review summarizes the recent works in developing RIPK2 inhibitors and degraders. We also briefly describe RIPK2 structure and its functions.
https://www.frontiersin.org/articles/10.3389/fphar.2023.1127722/full
#RIPK2 #medicinalchemistry #autoimmunedisease #drugdiscovery #kinase #inhibitors
Recent advances in the development of RIPK2 modulators for the treatment of inflammatory diseases
Receptor-interacting serine/threonine kinase 2 (RIPK2) is a vital immunomodulator that plays critical roles in nucleotide-binding oligomerization domain 1 (NOD1), NOD2, and Toll-like receptors (TLRs) signaling. Stimulated NOD1 and NOD2 interact with RIPK2 and lead to the activation of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK), followed by the production of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-12/23. Defects in NOD/RIPK2 signaling are associated with numerous inflammatory diseases, including asthma, sarcoidosis, inflammatory bowel disease (Crohn’s disease and ulcerative colitis), multiple sclerosis, and Blau syndrome. As RIPK2 is a crucial element of innate immunity, small molecules regulating RIPK2 functions are attractive to establish novel immunotherapies. The increased interest in developing RIPK2 inhibitors has led to the clinical investigations of novel drug candidates. In this review, we attempt to summarize recent advances in the development of RIPK2 inhibitors and degraders.