Vishal Pendharkar

TL;DR: Preclinical proof-of-concept that inhibiting mammalian Wnts can be achieved by targeting PORCN with small-molecule inhibitors such as C59 is offered, and that this is a safe and feasible strategy in vivo.

TL;DR: A novel potent, orally available PORCN inhibitor, ETC-1922159, that blocks the secretion and activity of all Wnts is developed that is remarkably effective in treating RSPO-translocation bearing colorectal cancer patient-derived xenografts.

TL;DR: It is proposed that p53 acts to prevent DNA topological stress originating from transcription during the S phase and, therefore, promotes normal replication fork progression, and Pharmacologic inhibition of transcription attenuates DNA damage and decreases Topo-II-DNA complexes, restoring cell viability in p53-deficient cells.

TL;DR: A structure- and biophysics-driven fragment-based ligand design strategy is applied to discover a novel family of potent inhibitors for human tankyrases, yielding compounds with affinities and IC50 values in the low nanomolar range and with good solubility, PARP selectivity, and ligand efficiency.

TL;DR: The first synthesis of BCP-resveratrol is described, which will have an inherently better in vivo PK profile as compared to its natural counterpart, and its PK properties are disclosed.