Discovery and development of antimitotic agents that inhibit tubulin polymerisation for the treatment of cancer

Q Li, HL Sham - Expert Opinion on Therapeutic Patents, 2002 - Taylor & Francis
Antimitotic agents have generated considerable interest among cytotoxic agents due to the
tremendous success of the taxanes and the widespread use of the Vinca alkaloids in clinical …

ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease

HL Sham, DJ Kempf, A Molla, KC Marsh… - Antimicrobial agents …, 1998 - Am Soc Microbiol
The valine at position 82 (Val 82) in the active site of the human immunodeficiency virus (HIV)
protease mutates in response to therapy with the protease inhibitor ritonavir. By using the X…

Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure− activity relationship, pharmacokinetics, and in vivo antitumor activity …

…, D Frost, SH Rosenberg, HL Sham - Journal of medicinal …, 2002 - ACS Publications
The synthesis and structure−activity relationship study of a series of compounds with
heterocycles in place of the cis double bond in combretastatin A-4 (CA-4) are described. …

Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy

DJ Kempf, HL Sham, KC Marsh… - Journal of medicinal …, 1998 - ACS Publications
The structure−activity studies leading to the potent and clinically efficacious HIV protease
inhibitor ritonavir are described. Beginning with the moderately potent and orally bioavailable …

[HTML][HTML] Polo-like kinase 2 (PLK2) phosphorylates α-synuclein at serine 129 in central nervous system

…, T Yednock, F Bard, GS Basi, H Sham… - Journal of Biological …, 2009 - ASBMB
Several neurological diseases, including Parkinson disease and dementia with Lewy bodies,
are characterized by the accumulation of α-synuclein phosphorylated at Ser-129 (p-Ser-…

Inhibition and catalytic mechanism of HIV-1 aspartic protease

AM Silva, RE Cachau, HL Sham, JW Erickson - Journal of molecular …, 1996 - Elsevier
The structure of the HIV-1 protease in complex with a pseudo-C2 symmetric inhibitor, which
contains a central difluoroketone motif, has been determined with X-ray diffraction data …

Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores

…, V Giranda, K Stewart, H Sham… - Journal of medicinal …, 2001 - ACS Publications
The discovery of (±)-(2S,3R,4R)-2-(trifluoroacetamido)methyl-3-amino-1-(N‘-ethyl-N‘-isopropylcarbamyl)pyrrolidine-4-carboxylic
acid (A-192558, 20e) as a potent inhibitor of influenza …

Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity

…, EH Fry, CW Hutchins, HL Sham… - Journal of medicinal …, 2006 - ACS Publications
The c-Jun N-terminal kinases (JNK-1, -2, and -3) are members of the mitogen activated protein
(MAP) kinase family of enzymes. They are activated in response to certain cytokines, as …

Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor

…, Z Su, GJ Diaz, CA Collins, H Sham… - Journal of medicinal …, 2008 - ACS Publications
A highly potent and selective DGAT-1 inhibitor was identified and used in rodent models of
obesity and postprandial chylomicron excursion to validate DGAT-1 inhibition as a novel …

Selective Chk1 inhibitors differentially sensitize p53‐deficient cancer cells to cancer therapeutics

…, ZF Tao, Y Tong, NH Lin, HL Sham… - … journal of cancer, 2006 - Wiley Online Library
The majority of cancer therapeutics induces DNA damage to kill cells. Normal proliferating
cells undergo cell cycle arrest in response to DNA damage, thus allowing DNA repair to …