[HTML][HTML] Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

…, RJ Colonno, DM Grasela, NA Meanwell, LG Hamann - Nature, 2010 - nature.com
The worldwide prevalence of chronic hepatitis C virus (HCV) infection is estimated to be
approaching 200 million people 1 . Current therapy relies upon a combination of pegylated …

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 …

…, MS Kirby, RA Parker, LG Hamann - Journal of medicinal …, 2005 - ACS Publications
Efforts to further elucidate structure−activity relationships (SAR) within our previously
disclosed series of β-quaternary amino acid linked l-cis-4,5-methanoprolinenitrile dipeptidyl …

Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists

…, ED Bischoff, RM Cesario, L Jow, LG Hamann… - Nature, 1997 - nature.com
Retinoic acid receptors (RAR), thyroid hormone receptors (TR), peroxisome proliferator
activated receptors (PPARs) and the orphan receptor, LXR, bind preferentially to DNA as …

Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo

…, PM Finan, MA Labow, X Mao, LG Hamann… - Nature cell …, 2014 - nature.com
Cells rely on autophagy to clear misfolded proteins and damaged organelles to maintain
cellular homeostasis. In this study we use the new autophagy inhibitor PIK-III to screen for …

SMN2 splice modulators enhance U1–pre-mRNA association and rescue SMA mice

…, JA Porter, VE Myer, JA Tallarico, LG Hamann… - Nature chemical …, 2015 - nature.com
Spinal muscular atrophy (SMA), which results from the loss of expression of the survival of
motor neuron-1 (SMN1) gene, represents the most common genetic cause of pediatric …

Thiazolidinediones repress ob gene expression in rodents via activation of peroxisome proliferator-activated receptor gamma.

…, K Wong, R Saladin, LG Hamann… - The Journal of …, 1996 - Am Soc Clin Investig
The ob gene product, leptin, is a signaling factor regulating body weight and energy balance.
ob gene expression in rodents is increased in obesity and is regulated by feeding patterns …

Development of targeted protein degradation therapeutics

PP Chamberlain, LG Hamann - Nature chemical biology, 2019 - nature.com
Targeted protein degradation as a therapeutic modality has seen dramatic progress and
massive investment in recent years because of the convergence of two key scientific …

SALL4 mediates teratogenicity as a thalidomide-dependent cereblon substrate

…, G Kumar, R Vessey, M Rolfe, LG Hamann… - Nature chemical …, 2018 - nature.com
Targeted protein degradation via small-molecule modulation of cereblon offers vast potential
for the development of new therapeutics. Cereblon-binding therapeutics carry the safety …

Sustainable practices in medicinal chemistry: current state and future directions

MC Bryan, B Dillon, LG Hamann… - Journal of medicinal …, 2013 - ACS Publications
The medicinal chemistry subgroup of the American Chemical Society’s Green Chemistry
Institute Pharmaceutical Roundtable (ACS GCI PR) offers a perspective on the current state of …

Discovery of CRBN E3 ligase modulator CC-92480 for the treatment of relapsed and refractory multiple myeloma

…, T Daniel, R Vessey, LG Hamann… - Journal of medicinal …, 2020 - ACS Publications
Many patients with multiple myeloma (MM) initially respond to treatment with modern combination
regimens including immunomodulatory agents (lenalidomide and pomalidomide) and …